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骨化三醇

骨化三醇用途

Calcitriol 是活性最大的 vitamin D 代谢物,也是 vitamin D 受体 (VDR) 的激动剂。

骨化三醇名称

[ CAS 号 ]:
32222-06-3

[ 中文名 ]:
骨化三醇

[ 英文名 ]:
Calcitriol

[中文别名 ]:

[英文别名 ]:

MFCD00867079
1α,25-Dihydroxyvitamin D3
EINECS 250-963-8

骨化三醇生物活性

[ 描述 ]:

Calcitriol 是活性最大的 vitamin D 代谢物,也是 vitamin D 受体 (VDR) 的激动剂。

[ 相关类别 ]:

信号通路 >> 维生素 D 相关 >> VD/VDR

研究领域 >> 癌症

天然产物 >> 其他

[ 靶点 ]

Human Endogenous Metabolite

[体外研究]

骨化三醇在体外对宫颈癌细胞发挥抗增殖作用。与对照相比,当用100nM Calcitriol处理6天时,细胞减少12.8％。随着骨化三醇浓度的增加,细胞增殖的抑制变得更加明显。 200和500 nM Calcitriol分别下降26.1％和31.6％。与对照组(24.36％)相比,用骨化三醇治疗72小时诱导细胞在G1期明显积累,200nM中约66.18％,500nM中78.10％。与对照相比,骨化三醇处理以时间和剂量依赖性方式显着降低HCCR-1蛋白表达[1]。骨化三醇以剂量依赖方式显着增加ERαmRNA,EC50为9.8×10-9 M [2]。

[体内研究]

用骨化三醇(150ng/kg每天,4.5个月)进行慢性治疗可改善松弛作用(骨化三醇治疗的OVX中pD2：6.30±0.09,Emax：68.6±3.9％,n = 8)。在两个肾脏中OVX大鼠的肾血流减少,并且通过骨化三醇治疗恢复血流。 OVX大鼠肾动脉中COX-2和血栓素-前列腺素(TP)受体的表达增加通过慢性钙三醇给药减少[3]。在第56天,高剂量和低剂量的Calcitriol治疗显着降低了果糖喂养大鼠的收缩压(SBP)14±4和9±4 mmHg。高剂量骨化三醇治疗(20 ng/kg /当天)与其他组相比,血清钙离子浓度显着升高(1.44±0.05 mmol/L)[4]。

[细胞实验]

将HeLa S3细胞以1,000个细胞/孔的密度接种在含有10％胎牛血清（FBS）的Dulbecco改良的Eagle培养基（DMEM）的96孔板中，用1％乙醇（对照）或各种浓度的Calcitriol处理（ 100,200和500nM）72小时。细胞计数试剂盒8（CCK-8）用于确定细胞增殖。在用200nM骨化三醇培养后24,48,72,96,120和144小时，收获细胞用于分析。一式三份进行三次独立实验[1]。

[动物实验]

在该研究中使用重200至220g的成年雌性Sprague-Dawley大鼠。将大鼠圈养在温控室（~23℃）中，12小时光照/黑暗循环。动物可以免费获得标准饮食和水。对大鼠进行卵巢切除术（OVX）。在外科手术后6个月，将OVX大鼠随机分配到用载体二甲基亚砜（OVX +载体）或骨化三醇（每天150ng / kg，OVX +骨化三醇）处理。通过口服强饲法给予骨化三醇治疗并持续或4.5个月。测量血压和血清骨化三醇水平[3]。

[参考文献]

[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.

[2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230.

[3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.

[4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843.

[相关活性小分子]

骨化三醇物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
565.0±50.0 °C at 760 mmHg

[ 熔点 ]:
119-1210C

[ 分子式 ]:
C₂₇H₄₄O₃

[ 分子量 ]:
416.637

[ 闪点 ]:
238.4±24.7 °C

[ 精确质量 ]:
416.329041

[ PSA ]:
60.69000

[ LogP ]:
6.12

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±3.5 mmHg at 25°C

[ 折射率 ]:
1.547

[ 储存条件 ]:
库房通风低温干燥,与食品分开储运

[ 稳定性 ]:
Air and Light Sensitive

骨化三醇MSDS

详细MSDS(安全技术说明书)

骨化三醇毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: FZ4645000

CHEMICAL NAME :: Cholecalciferol, 1-alpha,25-dihydroxy-

CAS REGISTRY NUMBER :: 32222-06-3

LAST UPDATED :: 199707

DATA ITEMS CITED :: 28

MOLECULAR FORMULA :: C27-H44-O3

MOLECULAR WEIGHT :: 416.71

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 :: 620 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - other changes

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 66 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 105 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1350 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1900 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 145 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 ug/kg/5W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 13650 ng/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - interstitial nephritis Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in potassium

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35100 ng/kg/26W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - conjunctive irritation Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Metabolism (Intermediary) - other proteins

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 9100 ng/kg/13W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 19960 ng/kg/52W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Kidney, Ureter, Bladder - interstitial nephritis Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 55 ug/kg

SEX/DURATION :: female 7-17 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 :: 15 ug/kg

SEX/DURATION :: female 16-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 9450 ng/kg

SEX/DURATION :: female 3 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - other effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 11550 ug/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating

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 - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 11550 ug/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 4950 ug/kg

SEX/DURATION :: female 7-17 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 :: Parenteral

DOSE :: 15 ug/kg

SEX/DURATION :: female 16-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 104 ng/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 520 ng/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

MUTATION DATA

TYPE OF TEST :: Unscheduled DNA synthesis

TEST SYSTEM :: Rodent - mouse Cells - not otherwise specified

DOSE/DURATION :: 5 ug/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 46,5582,1986 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4899 No. of Facilities: 8 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 239 (estimated) No. of Female Employees: 157 (estimated)

骨化三醇安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P280-P302 + P352 + P312-P304 + P340 + P312-P370 + P378-P403 + P235

[ 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+:Verytoxic;

[ 风险声明 (欧洲) ]:
R26/27/28;R63

[ 安全声明 (欧洲) ]:
S36/37/39-S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 1

[ WGK德国 ]:
3

[ RTECS号 ]:
FZ4645000

[ 包装等级 ]:
I

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2942000000

骨化三醇合成路线

详细合成路线

骨化三醇上下游产品

骨化三醇上游产品

骨化三醇下游产品

骨化三醇海关

[ 海关编码 ]: 2942000000

骨化三醇文献

1,25-dihydroxyvitamin D3 causes ADAM10-dependent ectodomain shedding of tumor necrosis factor receptor 1 in vascular smooth muscle cells.

Mol. Pharmacol. 87(3) , 533-42, (2015)

1,25-Dihydroxyvitamin D3 (1,25D3) has a potential antiatherosclerotic effect through anti-inflammatory actions. We investigated how 1,25D3 regulates tumor necrosis factor-α (TNF-α)-induced lectin-like...

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

更多文献

骨化三醇相关知识

[骨化三醇]-说明书-作用-骨化三醇胶丸副作用

2019-01-02 12:45:43

导读：骨化三醇的作用同维生素D3。口服吸收快，3～6小时达高峰，t1/2约3～6小时，经7小时后尿钙浓度增加，单次口服剂量可持续药理活性3～5日。应用于甲状旁腺功能低下症及血液透析患者的肾性营养不良。【药品名称】通用名称：骨化三醇胶丸商品名称：骨化三醇胶丸(罗盖全) 英文名称：Calci...