西司他丁钠

西司他丁钠用途

Cilastatin sodium (MK0791 sodium) 是一种可逆的竞争性的肾脏脱氢肽酶 I (renal dehydropeptidase I) 抑制剂,IC50 为 0.1 μM。Cilastatin sodium 抑制细菌金属叶内酰胺酶 CphA 的 IC50 为 178 μM。Cilastatin sodium 可用作抗菌辅助剂。

西司他丁钠名称

[ CAS 号 ]:
81129-83-1

[ 中文名 ]:
西司他丁钠

[ 英文名 ]:
Cilastatin Sodium

[中文别名 ]:

[英文别名 ]:

MFCD01723687
W-13 hydrochloride
Cilastatine
Cilastatin sodium salt
Cilastatin Sodium
Sodium Cilastatin
monosodiumsalt,(r-(r*,s*(z)))-)carbonyl)amino)
EINECS 279-694-4

西司他丁钠生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

IC50: 0.1 μM (Renal dehydropeptidase I); 178 μM (Bacterial metallob-lactamase enzyme CphA)[1]

[体外研究]

西司他丁(200μg/mL；24小时；RPTECs)治疗可防止万古霉素诱导的近端小管细胞凋亡,并提高细胞活力,同时不影响万古霉素的抗菌作用[2]。细胞凋亡分析[2]细胞系：肾近端小管上皮细胞(RPTECs)浓度：200μg/mL孵育时间：24h结果：万古霉素诱导的核细胞凋亡明显改善。

[体内研究]

在小鼠全身感染模型(雌性小鼠,株CD-1,20g)中,亚胺培南加西拉他丁可保护小鼠免受金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌感染[3]。

[参考文献]

[1]. Keynan S, et al. The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterialmetallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.

[2]. S Keynan, et al. The Renal Membrane Dipeptidase (Dehydropeptidase I) Inhibitor, Cilastatin, Inhibits the Bacterial Metallo-Beta-Lactamase Enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.

[3]. Blanca Humanes, et al. Protective Effects of Cilastatin Against Vancomycin-Induced Nephrotoxicity. Biomed Res Int. 2015;2015:704382.

[4]. P J Petersen, et al. In Vitro and in Vivo Activities of LJC10,627, a New Carbapenem With Stability to Dehydropeptidase I. Antimicrob Agents Chemother. 1991 Jan;35(1):203-7.

西司他丁钠物理化学性质

[ 沸点 ]:
655.5ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₂₅N₂NaO₅S

[ 分子量 ]:
380.43500

[ 闪点 ]:
350.2ºC

[ 精确质量 ]:
380.13800

[ PSA ]:
157.85000

[ LogP ]:
1.18910

[ 外观性状 ]:
一种白色色粉末

[ 储存条件 ]:
Desiccate at -20°C

西司他丁钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MJ9650200

CHEMICAL NAME :: 2-Heptenoic acid, 7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyc lopropyl)carbonyl) amino)-, monosodium salt, (R-(R*,S*(Z)))-

CAS REGISTRY NUMBER :: 81129-83-1

LAST UPDATED :: 199209

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C16-H25-N2-O5-S.Na

MOLECULAR WEIGHT :: 380.48

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 :: >10 gm/kg

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

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5027 mg/kg

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

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6786 mg/kg

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

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 33(Suppl 4),119,1985

西司他丁钠安全信息

[ 危害码 (欧洲) ]:
Xi

[ RTECS号 ]:
MJ9650200