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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Alternate Names: [R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2- [[(2,2-dimethylcyclopropyl)carbonyl]amino]-2- heptenoic acid monosodium salt
Application Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects
CAS 등록번호: 81129-83-1
순도: ≥98%
분자량: 380.43
분자식: C16H25N2O5S•Na
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).

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.


References

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

Physical State :
Solid
용해도 :
Soluble in water (25 mg/mL), DMSO (10 mg/mL), and methanol.
저장 :
Store at -20° C
Ki 데이타 :
LTDase: Ki= 0.11 µM; leukotriene D4 hydrolase: Ki= 0.11 µM; dehydropeptidase I: Ki= 0.11 µM
pK Values :
pKa: 2.0, 4.4, 9.2
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
RTECS :
MJ9650200
PubChem CID :
EC Number :
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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