Cilastatin sodium CAS: 81129-83-1
MF: C16H25N2O5S•Na
MW: 380.43
A dipeptidase inhibitor with nephroprotective effects.

Cilastatin sodium (CAS 81129-83-1)

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备用名: [R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2- [[(2,2-dimethylcyclopropyl)carbonyl]amino]-2- heptenoic acid monosodium salt
应用; Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects
CAS号码: 81129-83-1
纯度: ≥98%
分子量: 380.43
分子式: C16H25N2O5S•Na
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

Cilastatin is a dipeptidase inhibitor that specifically inhibits DPEP1 (dehydrodipeptidase I), a renal membrane-bound glycoprotein involved in the hydrolytic metabolism of penem and carbapenem β-lactam antibiotics. Cilastatin has been shown to inhibit leukotriene D4 hydrolase in porcine kidney microvillar membranes which inhibits the conversion of leukotriene D4 to leukotriene E4. Also, Cilastatin has been used to maintain the antibiotic activity of imipenem (sc-205350) through inhibiting dipeptidase activity. It has been reported that Cilastatin exhibits nephroprotective effects in cyclosporine A-induced nephrotoxicity in kidney proximal tubule epithelial cells and inhibits the bacterial metallo-β-lactamase, an enzyme responsible for bacterial resistance to β-lactam antibiotics.


参考文献

1. Keynan, S., et al. 1995. Antimicrob. Agents Chemother. 39: 1629-1631. PMID: 7492120
2. Yamaya, M., et al. 1998. Respir Physiol. 111: 101-109. PMID: 9496476
3. White, I.J., et al. 1999. Anal. Biochem. 268: 245-251. PMID: 10075814
4. Nitanai, Y., et al. 2002. J. Mol. Biol. 321: 177-184. PMID: 12144777
5. Tejedor, A., et al. 2007. Curr Med Res Opin. 23: 505-513. PMID: 17355732
6. Jia, B., et al. 2010. Chemotherapy. 56: 285-290. PMID: 20714145
7. Camano, S., et al. 2010. J. Pharmacol. Exp. Ther. 334: 419-429. PMID: 20435919
8. Zilberberg, M.D., et al. 2010. Surg Infect. PMID: 20666580

物理状态 :
Solid
溶解度 :
Soluble in water (25 mg/mL), DMSO (10 mg/mL), and methanol.
保存 :
Store at -20° C
Ki 数据 :
LTDase: Ki= 0.11 µM; leukotriene D4 hydrolase: Ki= 0.11 µM; dehydropeptidase I: Ki= 0.11 µM
pK值 :
pKa: 2.0, 4.4, 9.2
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
RTECS :
MJ9650200
PubChem CID :
EC号码 :
279-694-4
SMILES :
CC1(C[[email protected]@H]1C(=O)N/C(=C\\CCCCSC[[email protected]@H](C(=O)O)N)/C(=O)[O-])C.[Na+]

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