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Cilastatin

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Chemical Structure| 82009-34-5 同义名 : MK0791
CAS号 : 82009-34-5
货号 : A371776
分子式 : C16H26N2O5S
纯度 : 95%
分子量 : 358.453
MDL号 : MFCD00867379
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(292.93 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 12 mg/mL(33.48 mM),配合低频超声,并水浴加热至45℃助溶

1M NaOH: 100 mg/mL(278.98 mM),配合低频超声,并调节pH至11

动物实验配方:
生物活性
描述 Membrane dipeptidase is a glycoprotein involved in the hydrolysis of dipeptides and dehydropeptides. Cilastatin is a reversible, competitive inhibitor of dehydropeptidase I, a renal dipeptidase, with an IC50 value of 0.1μM. It also inhibits bacterial metallo-β-lactamase enzyme CphA with an IC50 value of 178 ± 11μM[4]. Cilastatin at 3 and 6 mg/mL significantly reduced the detachment of renal proximal tubular epithelial cells (RPTECs). Treatment with cilastatin also significantly ameliorated vancomycin-induced nuclear apoptosis of RPTECs[5]. Cilastatin in combination with imipenem protected female CD-1 mice from S. aureus, E. coli, and P. aeruginosa infection[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.39mL

27.90mL

5.58mL

2.79mL

参考文献

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

[3]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.

[4]Keynan S, Hooper NM, Felici A, Amicosante G, Turner AJ. 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. doi: 10.1128/AAC.39.7.1629

[5]Humanes B, Jado JC, Camaño S, López-Parra V, Torres AM, Álvarez-Sala LA, Cercenado E, Tejedor A, Lázaro A. Protective Effects of Cilastatin against Vancomycin-Induced Nephrotoxicity. Biomed Res Int. 2015;2015:704382. doi: 10.1155/2015/704382

[6]Petersen PJ, Jacobus NV, Weiss WJ, Testa RT. 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. doi: 10.1128/AAC.35.1.203