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地诺前列酮

地诺前列酮用途

Prostaglandin E2是一种激素样物质,参与广泛的身体功能,如平滑肌的收缩和松弛,血管的扩张和收缩,血压的控制和炎症的调节。

地诺前列酮名称

[ CAS 号 ]:
363-24-6

[ 中文名 ]:
地诺前列酮

[ 英文名 ]:
Dinoprostone

[中文别名 ]:

[英文别名 ]:

地诺前列酮生物活性

[ 描述 ]:

Prostaglandin E2是一种激素样物质,参与广泛的身体功能,如平滑肌的收缩和松弛,血管的扩张和收缩,血压的控制和炎症的调节。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体
天然产物 >> 酸和醛
研究领域 >> 心血管疾病

[ 靶点 ]

EP2 Receptor

Human Endogenous Metabolite


[体外研究]

PGE2显示对照射和未照射的T淋巴细胞的混合物中IL2产生的抑制。 PGE2(0.1-10μM)剂量依赖性地抑制IL2的产生.PGE2在抑制细胞活化的诱导期期间起作用。用PGE2预孵育T淋巴细胞诱导抑制IL 2产生和PHA增殖的细胞[1]。

[体内研究]

PGE2(0.3μg/ k,ip)显着降低了大鼠中甲基丙烯酸酯微珠的吞噬作用的腹膜巨噬细胞的数量[2]。 PGE2(0.1mg/min,ia)增加肾血流量。 PGE2产生肾血管阻力的双相变化,血管舒张开始于0.01mg/min并且最大为约3mg/min,而在使用的最高剂量(20mg/min)下,PGE2诱导肾血管收缩[3]。

[细胞实验]

在PGE处理的T细胞或培养基处理的T细胞存在下,将CM中的淋巴细胞(1×10 6个细胞/ mL)在微量培养板(100μL)中一式三份进行培养,并用PHA-P以各种促有丝分裂剂量进行刺激。 72小时后,用每孔1μCi[3H]胸苷(比活度5Ci / mM)脉冲培养物16至18小时,用微量沉淀器收集,干燥,并在液体闪烁计数器中计数。

[动物实验]

在整个研究中使用雄性Sprague Dawley大鼠(200-250g)。连续3天,实验组大鼠每天腹腔注射PGE2(0.3μg/ kg体重(BW)),前列腺素抑制剂甲钴胺(10 mg / kg BW)或前列腺素前体花生四烯酸(0.3μg/公斤BW)。为了确定0.3μg/ kg BW的脂肪酸是否产生非特异性作用,还将生物学上无活性的脂肪酸11,14,17-二十碳三烯酸给予一组大鼠。对照组中的大鼠接受相当体积(2.0mL / kg BW)的载体。在第三天,将3mL含有1.2×10 6个荧光甲基丙烯酸酯微珠/ mL PBS的悬浮液腹膜内(ip)注射到每只大鼠中。 6小时后,给所有动物腹膜内注射常规剂量的各自治疗。 19-22小时后收获腹膜渗出细胞。

[参考文献]

[1]. Chouaib S, et al. The mechanisms of inhibition of human IL 2 production. II. PGE2 induction of suppressor T lymphocytes. J Immunol. 1984 Apr;132(4):1851-7.

[2]. Fernandez-Repollet E, et al. In vivo effects of prostaglandin E2 and arachidonic acid on phagocytosis of fluorescent methacrylate microbeads by rat peritoneal macrophages. J Histochem Cytochem. 1982 May;30(5):466-70.

[3]. Haylor J, et al. Renal vasodilator activity of prostaglandin E2 in the rat anaesthetized with pentobarbitone. Br J Pharmacol. 1982 May;76(1):131-7.


[相关活性小分子]

3-甲基腺嘌呤 | 氢化可的松 | N-乙酰半胱氨酸 | 维生素A酸; 视黄酸 | 褪黑素 | 烟酰胺 | 5'-三磷酸腺苷 | 对乙酰氨基苯酚 | 列腺素 E1 | 去氢表雄酮 | 肾上腺酮 | 孕酮; 黄体素; 黄体酮 | 二十二碳六烯酸 | 辅酶I | P物质

地诺前列酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
530.1±50.0 °C at 760 mmHg

[ 熔点 ]:
66-68 °C

[ 分子式 ]:
C20H32O5

[ 分子量 ]:
352.465

[ 闪点 ]:
288.5±26.6 °C

[ 精确质量 ]:
352.224976

[ PSA ]:
94.83000

[ LogP ]:
1.88

[ 外观性状 ]:
白色晶体

[ 蒸汽压 ]:
0.0±3.2 mmHg at 25°C

[ 折射率 ]:
1.561

[ 储存条件 ]:
-20°C;避免加热

[ 水溶解性 ]:
insoluble

地诺前列酮MSDS

地诺前列酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UK8000000
CHEMICAL NAME :
Prosta-5,13-dien-1-oic acid, (5Z,11-alpha,13E,15S)-11,15-dihydroxy-9-oxo-
CAS REGISTRY NUMBER :
363-24-6
LAST UPDATED :
199603
DATA ITEMS CITED :
72
MOLECULAR FORMULA :
C20-H32-O5
MOLECULAR WEIGHT :
352.52
WISWESSER LINE NOTATION :
L5VTJ B2U4VQ C1U1YQ5 DQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
31600 ug/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
59500 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
19700 ug/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
23200 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - hamster
DOSE/DURATION :
1 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3360 mg/kg/4W-C
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in adrenal weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
200 ug/kg
SEX/DURATION :
lactating female 3 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - postpartum
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
16800 ug/kg
SEX/DURATION :
female 10 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
100 ng/kg
SEX/DURATION :
female 23 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
65 ug/kg
SEX/DURATION :
female 27 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
14400 ng/kg
SEX/DURATION :
female 15 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
500 ng/kg
SEX/DURATION :
female 8 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
400 ug/kg
SEX/DURATION :
female 16 week(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - uterus, cervix, vagina
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraplacental
DOSE :
100 ug/kg
SEX/DURATION :
female 15 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intracervical
DOSE :
10 ug/kg
SEX/DURATION :
female 42 week(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - uterus, cervix, vagina
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intracervical
DOSE :
48 ug/kg
SEX/DURATION :
female 14 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravaginal
DOSE :
2400 ug/kg
SEX/DURATION :
female 14 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravaginal
DOSE :
800 ug/kg
SEX/DURATION :
female 2 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1440 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravaginal
DOSE :
60 ug/kg
SEX/DURATION :
female 41 week(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
3600 ug/kg
SEX/DURATION :
female 20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - parturition
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
6 mg/kg
SEX/DURATION :
female 12-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - homeostasis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
75 mg/kg
SEX/DURATION :
female 6-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
1200 ug/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
2 mg/kg
SEX/DURATION :
female 15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
6 mg/kg
SEX/DURATION :
female 12-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - homeostasis Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
17500 ug/kg
SEX/DURATION :
female 1-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
30 mg/kg
SEX/DURATION :
female 1-6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
32 mg/kg
SEX/DURATION :
female 4-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
30 mg/kg
SEX/DURATION :
female 1-5 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
64 mg/kg
SEX/DURATION :
female 4-7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intratesticular
DOSE :
12 mg/kg
SEX/DURATION :
male 3 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intratesticular
DOSE :
4 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intratesticular
DOSE :
400 ug/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intrauterine
DOSE :
25 ug/kg
SEX/DURATION :
female 5 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
36 mg/kg
SEX/DURATION :
female 7-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1440 mg/kg
SEX/DURATION :
female 7-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - sex ratio
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
720 mg/kg
SEX/DURATION :
female 7-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
30 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
60 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
150 mg/kg
SEX/DURATION :
female 6-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
5 mg/kg
SEX/DURATION :
female 16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
746 ug/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - urogenital system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
746 ug/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
30 mg/kg
SEX/DURATION :
male 15 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
2 mg/kg
SEX/DURATION :
female 5-6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
20 ug/kg
SEX/DURATION :
female 16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
18 mg/kg
SEX/DURATION :
female 21-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
3 mg/kg
SEX/DURATION :
female 1 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
22500 ug/kg
SEX/DURATION :
female 1-3 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
2 mg/kg
SEX/DURATION :
female 1 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
4 mg/kg
SEX/DURATION :
female 23-24 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
48 mg/kg
SEX/DURATION :
female 4-6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
200 ug/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
500 ug/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
1 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
800 ug/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
800 ug/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Specific Developmental Abnormalities - homeostasis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
800 ug/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1600 ug/kg
SEX/DURATION :
female 5 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
3600 ug/kg
SEX/DURATION :
female 4-6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intracervical
DOSE :
48 ug/kg
SEX/DURATION :
female 33-44 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - uterus, cervix, vagina
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravaginal
DOSE :
4 ug/kg
SEX/DURATION :
female 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - uterus, cervix, vagina
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Sperm Morphology

MUTATION DATA

TYPE OF TEST :
Unscheduled DNA synthesis
TEST SYSTEM :
Rodent - guinea pig Lung
DOSE/DURATION :
1 mg/L
REFERENCE :
PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 171,109,1982 *** REVIEWS *** TOXICOLOGY REVIEW CSPEAX Cosmetics and Perfumery. (Oak Park, IL) V.88-90, 1973-75. For publisher information, see CTOIDG. Volume(issue)/page/year: 90(12),28,1975 TOXICOLOGY REVIEW AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 113,130,1972

地诺前列酮安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H360

[ 警示性声明 ]:
P201-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R60;R22

[ 安全声明 (欧洲) ]:
S53-S22-S26-S36/37/39

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UK8000000

地诺前列酮合成路线

地诺前列酮上下游产品

地诺前列酮制备

以羊精囊为原料
反应液的制备 取-30℃冷藏的羊精囊,除去结缔组织及脂肪,每1kg加1L 0.154mol/L氯化钾溶液,在4000r/min下离心25min,取上清液,过滤,得清液。残渣加氯化钾再提取一次,离心过滤后,合并二次上清液。加2mol/L枸橼酸调pH5,在4000r/min下离心25min,弃上清液,加100 ml 0.2mol/L磷酸盐缓冲液洗下沉淀,再加100ml 6.2.5×10-5 mol/L EDTA溶液搅匀,加2mol/L氢氧化钾调pH8,得酶混悬液。取酶的混悬液,每升加氢醌40mg、加GSH 500mg,先用少量水溶解后,加入酶的混悬液中,再将1kg羊精囊加1g AA,搅拌通氧,升温至37-38℃,孵育1h,得反应液。
绵羊精囊[pH8]→[KCl, EDTA Na2]酶混悬液[氢醌,谷胱甘肽]→[花生四烯酸,O2]反应液
PGE粗品的制备 将反应液加丙酮(第一次3倍量,第二次2倍量)提取两次,每次0.5-1h,过滤,合并两次滤液,45℃减压浓缩或薄膜浓缩,得浓缩液。加4mol/L盐酸调pH 3,加乙醚、0.2mol/L磷酸盐缓冲液、石油醚分别萃取3次,取水层,加4mol/L盐酸调pH 3,加二氯甲烷萃取3次,二氯甲烷层经水洗、无水硫酸钠脱水后,密塞置冰箱中过夜,过滤,40℃以下减压浓缩得黄色油状物,即PGS粗品。每1g PGS粗品用15g 100-160目活化硅胶,湿法装柱。将PGS粗品溶解于少量氯仿,过柱层析分离,依次以氯仿、V氯仿:V甲醇=98:2、 V氯仿:V甲醇=96:4三种溶液洗脱,收集洗脱液,硅胶柱层析鉴定,相同洗脱液合并,得PGA和PGE部分。将PGE洗脱液在35℃以下浓缩,得PGE粗品。
反应液[丙酮,乙醚,二氯甲烷]→PGS粗品[硅胶柱]→PGE粗品
APGE2成品的制备 每1g PGE粗品用20g硅胶,取200-250目10倍PGE质量的活化硝酸银硅胶混悬于V乙酸乙酯:V冰醋酸:V石油醚:V=220:22.5:125:5(石油醚的bp 90-120℃)的展开剂中。湿法装柱,将粗品用少量的同一展开剂溶解,上柱,洗脱。分别收集PGE1和PGE2部分。将PGE2部分于35℃以下充氮浓缩至无醋酸味,加乙酸乙酯溶解,加水洗酸,pH4-5,加生理盐水除银。乙酸乙酯溶液加无水硫酸钠干燥,充氮,密塞,置冰箱过夜,过滤,滤液于35℃以下充氮浓缩,得PGE2精晶,经乙酸乙酯-己烷重结晶2次,得PGE2成品。
PGE粗品[硝酸银硅胶柱]→PGE2(油)[乙酸乙酯-己烷]→PGE2

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MLN4924 sensitizes monocytes and maturing dendritic cells for TNF-dependent and -independent necroptosis.

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公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

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