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22862-76-6生产厂家

22862-76-6价格

22862-76-6

22862-76-6结构式
22862-76-6结构式
  • 常用中文名:茴香霉素
  • 常用英文名:Anisomycin
  • CAS号:22862-76-6
  • 分子式:C14H19NO4
  • 分子量:265.305
  • 相关类别: 原料药 抗生素类药物 其它抗生素类药
  • 发布时间:2018-02-11 08:00:00
  • 更新时间:2024-01-02 18:43:09
  • Anisomycin是一种有效的蛋白质合成抑制剂,它通过抑制肽基转移酶或80S核糖体系统干扰蛋白质和DNA合成。

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中文名 茴香霉素
英文名 (-)-anisomycin
英文别名 antibioticpa-106
(2S,3R,4R)-4-Hydroxy-2-(4-methoxybenzyl)-3-pyrrolidinyl acetate
(2S,3R,4R)-4-Hydroxy-2-(4-methoxybenzyl)pyrrolidin-3-yl acetate
[2R-(2a,3a,4b)]-2-[(4-Methoxyphenyl)methyl]-3,4-pyrrolidinediol 3-Acetate
ANISOMYCIN,STREPTOMYCES GRISEOLUS
EINECS 245-269-7
MFCD00077650
Anisomycin
Anisomycin,(2R,3S,4S)-2-[(4-Methoxyphenyl)methyl]-3,4-pyrrolidinediol3-acetate
FLAGECIDIN
Anisomycin from Streptomyces griseolus
2-p-methoxyphenylmethyl-3-acetoxy-4-hydroxypyrrolidine
3,4-Pyrrolidinediol, 2-[(4-methoxyphenyl)methyl]-, 3-acetate, (2S,3R,4R)-
(2R,3S,4S)-2-(4-Methoxybenzyl)-3,4-pyrrolidinediol 3-Acetate
描述 Anisomycin是一种有效的蛋白质合成抑制剂,它通过抑制肽基转移酶或80S核糖体系统干扰蛋白质和DNA合成。
相关类别
靶点

DNA synthesis[1]

体外研究 为了检查JNK是否在PC-12细胞中的粘菌素诱导的神经毒性中具有核心作用,在该研究中使用SP600125(JNK的高选择性抑制剂)和Anisomycin(强效激活剂)。为了选择合适的浓度,分别用一系列SP600125(0-80μM)和Anisomycin(0-20μM)处理PC-12细胞24小时。结果显示,SP600125处理以浓度依赖性方式显着降低细胞存活率,在大于20μM的浓度下观察到(p <0.01)。类似地,通过Anisomycin处理(≥8μM)抑制细胞活力(p <0.05)[1]。
体内研究 TNFRp55/p75的破坏减弱了Anisomycin诱导的心室功能改善。 Anisomycin导致左心室发展压力(LVDP)的改善,其在TNFR p55/p75破坏的动物中消失。此外,通过删除TNFR p55/p75消除了野生型动物中的Anisomycin诱导的LVEDP改善。同样地,TNFR p55/p75的破坏消除了通过预处理Anisomycin引起的速率压力产物(RPP)的回收。与对照野生型小鼠相比,没有使用Anisomycin处理的TNFR p55/p75 -/-小鼠在心脏功能恢复方面没有显示出差异。野生型和TNFR p55/p75缺陷小鼠的心率没有显着差异。为了观察Nox2是否参与Anisomycin诱导的心肌保护,用Anisomycin处理Nox2缺陷型小鼠。与野生型小鼠相比,在Nox2 -/-小鼠中消除了在Anisomycin处理的小鼠中LVEDP的改善。此外,在Nox2 -/-小鼠中减轻了用Anisomycin处理的野生型小鼠中RPP的恢复。与野生型对照小鼠相比,没有使用Anisomycin处理的Nox2 -/-小鼠在心脏功能恢复方面没有显示出差异[2]。
细胞实验 将PC-12细胞以1×10 4个细胞/孔的浓度接种于96孔板中,并在37℃,5%CO 2的培养箱中培养至少12小时,然后暴露于不同浓度的SP600125(0- 80μM)或Anisomycin(0-20μM)24小时。随后,将培养基加入20μL5mg/ mL MTT工作溶液中,并将板在37℃下温育2小时。除去培养上清液,将甲crystals晶体溶于150μLDMSO中。最后,通过酶标仪在490nm处测量每个孔的吸光度。细胞活力表示为对照组的百分比,设定为100%[1]。
动物实验 小鼠[2]在该研究中使用成年雄性TNFRp55 / p75小鼠,成年雄性野生型C57 / BL和纯合型Nox2 - / - 小鼠。将小鼠随机分成六个实验组,进行以下治疗。将动物分为六组:第1组:对照缺血/再灌注,向野生型小鼠注射DMSO(0.1mL);第2组:Anisomycin +野生型小鼠,野生型小鼠注射Anisomycin(0.1 mg / kg ip);组3:Anisomycin + TNFR p55 / p75 - / - 小鼠,TNFR p55 / 75 - / - 小鼠注射Anisomycin(0.1mg / kg ip);第4组:TNFR p55 / p75 - / - 小鼠,TNFR p55 / 75 - / - 小鼠未注射Anisomycin;组5:Anisomycin + Nox2 - / - 小鼠,Nox2 - / - 小鼠注射Anisomycin(0.1mg / kg ip);和第6组:Nox2 - / - 小鼠,Nox2 - / - 小鼠未注射Anisomycin。后来(24小时),心脏缺血30分钟,再灌注30分钟[2]。
参考文献

[1]. Lu Z, et al. Colistin-induced autophagy and apoptosis involves the JNK-Bcl2-Bax signaling pathway and JNK-p53-ROS positive feedback loop in PC-12 cells.

[2]. Zhao TC, et al. Disruption of Nox2 and TNFRp55/p75 eliminates cardioprotection induced by Anisomycin. Am J Physiol Heart Circ Physiol. 2012 Nov 15;303(10):H1263-72.

密度 1.2±0.1 g/cm3
沸点 398.7±42.0 °C at 760 mmHg
熔点 140-141ºC
分子式 C14H19NO4
分子量 265.305
闪点 194.9±27.9 °C
精确质量 265.131409
PSA 67.79000
LogP 0.42
外观性状 白色结晶固体
蒸汽压 0.0±1.0 mmHg at 25°C
折射率 1.558
储存条件

放入紧密的贮藏器内,储存在阴凉,干燥的地方

稳定性

常温常压下稳定

避免接触 强氧化剂
分子结构

1、 摩尔折射率:70.46

2、 摩尔体积(cm3/mol):218.6

3、 等张比容(90.2K):577.8

4、 表面张力(dyne/cm):48.7

5、 极化率(10-24cm3):27.93

计算化学

1、疏水参数计算参考值(XlogP):0.9

2、氢键供体数量:2

3、氢键受体数量:5

4、可旋转化学键数量:5

5、互变异构体数量:

6、拓扑分子极性表面积(TPSA):67.8

7、重原子数量:19

8、表面电荷:0

9、复杂度:302

10、同位素原子数量:0

11、确定原子立构中心数量:3

12、不确定原子立构中心数量:0

13、确定化学键立构中心数量:0

14、不确定化学键立构中心数量:0

15、共价键单元数量:1

更多

1. 性状:长针状结晶。

2. 密度(g/mL,25/4℃): 未确定

3. 相对蒸汽密度(g/mL,空气=1):未确定

4. 熔点(ºC):140~141

5. 沸点(ºC,常压):未确定

6. 沸点(ºC,5.2kPa):未确定

7. 折射率:未确定

8. 闪点(ºC):未确定

9. 比旋光度(º,C=1,甲醇中):-30°

10. 自燃点或引燃温度(ºC):未确定

11. 蒸气压(kPa,25ºC):未确定

12. 饱和蒸气压(kPa,60ºC):未确定

13. 燃烧热(KJ/mol):未确定

14. 临界温度(ºC):未确定

15. 临界压力(KPa):未确定

16. 油水(辛醇/水)分配系数的对数值:未确定

17. 爆炸上限(%,V/V):未确定

18. 爆炸下限(%,V/V):未确定

19. 溶解性:溶于水、低级醇、酯、酮和氯仿,微溶于苯、甲苯和己烷。室温时水溶液在很宽的pH范围内稳定。

毒理学数据:


生态学数据:


CHEMICAL IDENTIFICATION

RTECS NUMBER :
BZ9800000
CHEMICAL NAME :
Anisomycin
CAS REGISTRY NUMBER :
22862-76-6
BEILSTEIN REFERENCE NO. :
0020705
LAST UPDATED :
199612
DATA ITEMS CITED :
18
MOLECULAR FORMULA :
C14-H19-N-O4
MOLECULAR WEIGHT :
265.34
WISWESSER LINE NOTATION :
T5MTJ B1R DO1& COV1 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 :
72 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
345 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
230 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
167 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
148 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
400 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
600 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
10 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,77,1981
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>300 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>100 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>100 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>300 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>50 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
>200 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5265 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 504 (estimated) No. of Female Employees: 420 (estimated)

符号 GHS06
GHS06
信号词 Danger
危害声明 H301
警示性声明 P301 + P310
个人防护装备 Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
危害码 (欧洲) T: Toxic;
风险声明 (欧洲) R25
安全声明 (欧洲) 45-36-26
危险品运输编码 UN 3462 6
WGK德国 3
RTECS号 BZ9800000
包装等级 III
危险类别 6.1(b)
海关编码 2933990090


海关编码 2933990090
中文概述 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%