For research use only. Not for therapeutic Use.
Cilastatin（Cat No.:R008363）is a renal dehydropeptidase-I (DHP-I) inhibitor used in combination with the antibiotic imipenem to enhance its effectiveness. By inhibiting the DHP-I enzyme in the kidneys, cilastatin prevents the degradation of imipenem, allowing higher concentrations of the antibiotic to remain in the body for a longer period. This combination is essential for treating severe bacterial infections, particularly those caused by resistant organisms. Cilastatin itself has no antibacterial activity but plays a crucial role in extending imipenem’s spectrum and duration of action, improving its efficacy in treating life-threatening infections.
| Catalog Number | R008363 |
| CAS Number | 82009-34-5 |
| Synonyms | (2Z)-7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic Acid;MK-791; |
| Molecular Formula | C₁₆H₂₆N₂O₅S |
| Purity | 95% |
| Target | class A and C β-lactamases |
| Target Protein | P0AD65 |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IUPAC Name | (Z)-7-[(2R)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid |
| InChI | InChI=1S/C16H26N2O5S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23)/b12-6-/t10-,11+/m1/s1 |
| InChIKey | DHSUYTOATWAVLW-WFVMDLQDSA-N |
| SMILES | CC1(C[C@@H]1C(=O)N/C(=C\CCCCSC[C@@H](C(=O)O)N)/C(=O)O)C |
| Reference | </br>1:Imipenem/cilastatin encapsulated polymeric nanoparticles for destroying carbapenem-resistant bacterial isolates. Shaaban MI, Shaker MA, Mady FM.J Nanobiotechnology. 2017 Apr 11;15(1):29. doi: 10.1186/s12951-017-0262-9. PMID: 28399890 Free PMC Article</br>2:Cisplatin-induced renal inflammation is ameliorated by cilastatin nephroprotection. Humanes B, Camaño S, Lara JM, Sabbisetti V, González-Nicolás MÁ, Bonventre JV, Tejedor A, Lázaro A.Nephrol Dial Transplant. 2017 Mar 11. doi: 10.1093/ndt/gfx005. [Epub ahead of print] PMID: 28340076 </br>3:Megalin Blockade with Cilastatin Suppresses Drug-Induced Nephrotoxicity. Hori Y, Aoki N, Kuwahara S, Hosojima M, Kaseda R, Goto S, Iida T, De S, Kabasawa H, Kaneko R, Aoki H, Tanabe Y, Kagamu H, Narita I, Kikuchi T, Saito A.J Am Soc Nephrol. 2017 Jan 4. pii: ASN.2016060606. doi: 10.1681/ASN.2016060606. [Epub ahead of print] PMID: 28052987 </br>4:Pharmacokinetics of Imipenem/Cilastatin Burn Intensive Care Unit Patients Undergoing High-Dose Continuous Venovenous Hemofiltration. Boucher BA, Hudson JQ, Hill DM, Swanson JM, Wood GC, Laizure SC, Arnold-Ross A, Hu ZY, Hickerson WL.Pharmacotherapy. 2016 Dec;36(12):1229-1237. doi: 10.1002/phar.1866. Epub 2016 Dec 4. PMID: 27862103 </br>5:Cilastatin does not affect Carba NP test performance for detection of carbapenemase production in Enterobacteriaceae. Hartl R, Widhalm S, Kerschner H, Apfalter P, Gattringer R.Wien Klin Wochenschr. 2017 Jan;129(1-2):29-32. doi: 10.1007/s00508-016-1106-6. Epub 2016 Oct 28. PMID: 27796502 </br>6:A novel chitosan-polyethylene oxide nanofibrous mat designed for controlled co-release of hydrocortisone and imipenem/cilastatin drugs. Fazli Y, Shariatinia Z, Kohsari I, Azadmehr A, Pourmortazavi SM.Int J Pharm. 2016 Nov 20;513(1-2):636-647. doi: 10.1016/j.ijpharm.2016.09.078. Epub 2016 Sep 29. PMID: 27693735 </br>7:Phase 2, Dose-Ranging Study of Relebactam with Imipenem-Cilastatin in Subjects with Complicated Intra-abdominal Infection. Lucasti C, Vasile L, Sandesc D, Venskutonis D, McLeroth P, Lala M, Rizk ML, Brown ML, Losada MC, Pedley A, Kartsonis NA, Paschke A.Antimicrob Agents Chemother. 2016 Sep 23;60(10):6234-43. doi: 10.1128/AAC.00633-16. Print 2016 Oct. PMID: 27503659 Free PMC Article</br>8:The Effect of Different Carbapenem Antibiotics (Ertapenem, Imipenem/Cilastatin, and Meropenem) on Serum Valproic Acid Concentrations. Wu CC, Pai TY, Hsiao FY, Shen LJ, Wu FL.Ther Drug Monit. 2016 Oct;38(5):587-92. doi: 10.1097/FTD.0000000000000316. PMID: 27322166 </br>9:Imipenem-cilastatin-induced psychosis: a case report. Ninan J, George GM.J Med Case Rep. 2016 Apr 27;10(1):107. doi: 10.1186/s13256-016-0883-x. PMID: 27118305 Free PMC Article</br>10:Imipenem/cilastatin-induced acute eosinophilic pneumonia. Foong KS, Lee A, Pekez M, Bin W.BMJ Case Rep. 2016 Mar 4;2016. pii: bcr2016214804. doi: 10.1136/bcr-2016-214804. PMID: 26944380 |
