Cilastatin sodium
- Product Name
- Cilastatin sodium
- CAS No.
- 81129-83-1
- Chemical Name
- Cilastatin sodium
- Synonyms
- l642957;Cilastatine;Sodium Cilastatin;Cilastatin sodium;Cilastatin Impurity 9;Cilastatin sodium CRS;Cilastatin sodium (C2170000);Cilastatin sodium Ready Made Solution;Cilastatin for system suitability 2 CRS;Cilastatin for system suitability 1 CRS
- CBNumber
- CB8260633
- Molecular Formula
- C16H25N2O5S.Na
- Formula Weight
- 380.44
- MOL File
- 81129-83-1.mol
Cilastatin sodium Property
- Melting point:
- >160°C (dec.)
- Flash point:
- 87℃
- storage temp.
- 2-8°C
- solubility
- Very soluble in water and in methanol, slightly soluble in anhydrous ethanol, very slightly soluble in dimethyl sulfoxide, practically insoluble in acetone and in methylene chloride.
- form
- Solid
- pka
- pKa1 2.0; pKa2 4.4; pKa3 9.2(at 25℃)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
- CAS DataBase Reference
- 81129-83-1(CAS DataBase Reference)
Safety
- RTECS
- MJ9650200
- HS Code
- 2941.90.1050
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML1283
- Product name
- Cilastatin sodium Ready Made Solution
- Purity
- 50 mg/mL in H2O
- Packaging
- 2ml
- Price
- $207
- Updated
- 2024/03/01
- Product number
- C5743
- Product name
- Cilastatin sodium salt
- Purity
- ≥98%(HPLC)
- Packaging
- 100mg
- Price
- $364
- Updated
- 2024/03/01
- Product number
- C2170000
- Product name
- Cilastatin sodium
- Purity
- European Pharmacopoeia (EP) Reference Standard
- Packaging
- c2170000
- Price
- $220
- Updated
- 2024/03/01
- Product number
- C3547
- Product name
- Cilastatin Sodium Salt
- Packaging
- 50MG
- Price
- $110
- Updated
- 2024/03/01
- Product number
- C441133
- Product name
- Cilastatin sodium
- Packaging
- 500mg
- Price
- $525
- Updated
- 2021/12/16
Cilastatin sodium Chemical Properties,Usage,Production
Description
Cilastatin Na (81129-83-1) is a dehydropeptidase-1 inhibitor. Inhibits the proteolytic conversion of leukotriene D4?to E4.1? Inhibits the mammalian β-lactamase renal dipeptidase (dehydropeptidase-1, DPEP1) and thus is used as an antibacterial adjunct to extend the half-life of β-lactam antibiotics.2?Cilastatin also inhibits bacterial metallo-β-lactamase and thereby may block resistance to the carbapenem family of antibiotics in certain bacteria.3? Suppresses invasion and metastasis of DPEP1-expressing tumor cells.4
Chemical Properties
White or light yellow amorphous, hygroscopic powder.
Uses
Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects.
Uses
Enzyme inhibitor.
Definition
ChEBI: The monosodium salt of cilastatin. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin sodium is therefore administ red with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to microbiologically inactive and potentially nephrotoxic products.
General Description
Cilastatin sodium salt is off-white to yellowish-white, hygroscopic, amorphous compound. It is derivatized from heptenoic acid. Its molecular mass is 380.43 g.
Biological Activity
Dipeptidase inhibitor (LTDase, leukotriene D4 hydrolase, dehydropeptidase I) that displays a K i value of 0.11 μ M. Inhibits metabolism of LTD 4 to LTE 4 and the hydrolysis of β -lactam antibiotics. Nephroprotective; reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells.
Biochem/physiol Actions
Inhibitor of the renal enzyme dehydropeptidase I and some bacterial zinc-containing β-lactamases. By these action, cilastatin suppresses both host and target metabolism of the broad-spectrum antibiotic imipenem, improving its efficacy.
References
1) White?et al.?(1999),?A continuous fluorometric assay for Leukotriene D4 hydrolase; Anal. Biochem.,?268?245 2) Graham?et al.?(1987),?Inhibition of the mammalian beta-lactamase renal dipeptidase (dehydropeptidase-I) by (Z)-2-acylamino-3-substituted propenoic acids; J. Med. Chem.,?30?1074 3) Keynan?et al. (1995),?The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA; Antimicreob. Agents Chemother.,?39?1629 4) Park?et al.?(2016),?Dehydropeptidase 1 promotes metastasis through regulation of E-cadherin expression in colon cancer; Oncotarget,?7?9501
Cilastatin sodium Preparation Products And Raw materials
Raw materials
Preparation Products
Cilastatin sodium Suppliers
- Tel
- 320-37350700
- Fax
- +32 (0)37350701
- sales@tcieurope.eu
- Country
- Europe
- ProdList
- 23671
- Advantage
- 75
- Tel
- --
- Fax
- --
- export@ecochem.dk
- Country
- Europe
- ProdList
- 6371
- Advantage
- 66
- Tel
- --
- Fax
- --
- Sales@kemikalieimport.dk
- Country
- Europe
- ProdList
- 6685
- Advantage
- 47
View Lastest Price from Cilastatin sodium manufacturers
- Product
- Cilastatin sodium 81129-83-1
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 98%min
- Supply Ability
- 30tons/month
- Release date
- 2023-01-29
- Product
- Cilastatin Sodium 81129-83-1
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 10000kg
- Release date
- 2024-05-07
- Product
- Cilastatin Sodium 81129-83-1
- Price
- US $11.00/g
- Min. Order
- 1g
- Purity
- 98%HPLC
- Supply Ability
- 20KG
- Release date
- 2023-06-13