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Cilastatin sodium

Cilastatin sodium Structure
Cilastatin sodium structure
CAS No.
81129-83-1
Chemical Name:
Cilastatin sodium
Synonyms
l642957;Cilastatine;Cilastatin sodium;Sodium Cilastatin;Cilastatin sodium CRS;Cilastatin Impurity 9;Cilastatin sodium (C2170000);13C3,2H3,15N]-Cilastatin sodium;Cilastatin sodium Ready Made Solution;Cilastatin for system suitability 2 CRS
CBNumber:
CB8260633
Molecular Formula:
C16H25N2O5S.Na
Molecular Weight:
380.44
MDL Number:
MFCD08459332
MOL File:
81129-83-1.mol
MSDS File:
SDS
Last updated:2023-06-13 18:01:23
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Cilastatin sodium Properties

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.
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)
FDA UNII 5428WXZ74M

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H319
Precautionary statements  P264-P280-P305+P351+P338-P337+P313P
RTECS  MJ9650200
HS Code  2941.90.1050

Cilastatin sodium price More Price(25)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1283 Cilastatin sodium Ready Made Solution 50 mg/mL in H2O 81129-83-1 2ml $207 2024-03-01 Buy
Sigma-Aldrich C5743 Cilastatin sodium salt ≥98%(HPLC) 81129-83-1 100mg $364 2024-03-01 Buy
Sigma-Aldrich C2170000 Cilastatin sodium European Pharmacopoeia (EP) Reference Standard 81129-83-1 c2170000 $220 2024-03-01 Buy
TCI Chemical C3547 Cilastatin Sodium Salt 81129-83-1 50MG $110 2024-03-01 Buy
TRC C441133 Cilastatin sodium 81129-83-1 500mg $525 2021-12-16 Buy
Product number Packaging Price Buy
SML1283 2ml $207 Buy
C5743 100mg $364 Buy
C2170000 c2170000 $220 Buy
C3547 50MG $110 Buy
C441133 500mg $525 Buy

Cilastatin sodium Chemical Properties,Uses,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

Enzyme inhibitor.

Uses

Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects.

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

Global( 163)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Standardpharm Co. Ltd. 		86-714-3992388 overseasales1@yongstandards.com United States 14336 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 47465 58
career henan chemical co 		+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
AFINE CHEMICALS LIMITED 		0571-85134551 info@afinechem.com CHINA 15377 58
Wuhan Fortuna Chemical Co., Ltd 		+86-27-59207850 +86-13986145403 info@fortunachem.com China 5985 58
Baoji Guokang Healthchem co.,ltd 		+8615604608665 15604608665 dominicguo@gk-bio.com CHINA 9427 58
Dayang Chem (Hangzhou) Co.,Ltd. 		571-88938639 +8617705817739 info@dycnchem.com CHINA 52867 58
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
Standardpharm Co. Ltd. 		58
BOC Sciences 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
TargetMol Chemicals Inc. 		58
AFINE CHEMICALS LIMITED 		58
Wuhan Fortuna Chemical Co., Ltd 		58
Baoji Guokang Healthchem co.,ltd 		58
Dayang Chem (Hangzhou) Co.,Ltd. 		58

View Lastest Price from Cilastatin sodium manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Cilastatin Sodium pictures 2024-03-20 Cilastatin Sodium
81129-83-1
 US $11.00 / g 1g 98%HPLC 20KG Wuhan Topule Biopharmaceutical Co., Ltd
Cilastatin sodium pictures 2023-01-30 Cilastatin sodium
81129-83-1
 US $0.00 / KG 1KG 98%min 30tons/month WUHAN FORTUNA CHEMICAL CO., LTD
Cilastatin sodium pictures 2020-02-18 Cilastatin sodium
81129-83-1
 US $1.00 / KG 1KG 99% 200kgs Career Henan Chemical Co
  • Cilastatin Sodium pictures
  • Cilastatin Sodium
    81129-83-1
  • US $11.00 / g
  • 98%HPLC
  • Wuhan Topule Biopharmaceutical Co., Ltd

81129-83-1(Cilastatin sodium)Related Search:

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Cilastatine Cilastatin sodium Sodium 7-(2-amino-2-carboxy-ethyl)sulfanyl-2-(2,2-dimethylcyclopropyl)carbonylamino-hept-2-enoate Sodium hydrogen 7-[(2-amino-2-carboxylatoethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]hept-2-enoate Sodium Cilastatin [R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]-2-heptenoic acid monosodium salt (Z)-7-[(R)-2-Amino-2-carboxyethylthio]-2-[(S)-2,2-dimethylcyclopropylcarbonylamino]-2-heptenoic acid 1-sodium salt (2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoicacidsodiumsalt 2-Heptenoicacid,7-[[(2R)-2-aMino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-diMethylcyclopropyl]carbonyl]aMino]-,sodiuM salt (1:1), (2Z)- Cilastatin sodium Ready Made Solution 2-heptenoicacid,7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyclopropyl l642957 monosodiumsalt,(r-(r*,s*(z)))-)carbonyl)amino) sodium hydrogen [R-[R*,S*-(Z)]]-7-[(2-amino-2-carboxylatoethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]hept-2-enoate Cilastatin sodium CRS Cilastatin for system suitability 2 CRS Cilastatin for system suitability 1 CRS sodium (Z)-7-(((R)-2-amino-2-carboxyethyl)thio)-2-((S)-2,2-dimethylcyclopropanecarboxamido)hept-2-enoate (R)-2-Amino-3-[[(Z)-6-carboxy-6-[(S)-2,2-dimethylcyclopropanecarboxamido]hex-5-en-1-yl]thio]propanoic Acid Monosodium Salt Monosodium (R)-2-Amino-3-[[(Z)-6-carboxy-6-[(S)-2,2-dimethylcyclopropanecarboxamido]hex-5-en-1-yl]thio]propanoate Sodium (Z)-7-(((R)-2-amino-2-carboxyethyl)thio)-2-((S)-2,2-dimethylcyclopropane-1-carboxamido)hept-2-enoate Cilastatin Impurity 9 Cilastatin sodium (C2170000) Sod i um (Z)-7-[[(2R)-2-a mi no-2-c a rb oxye th yl]sulf a nyl]-2-[[[(1S)-2,2-d i me th ylc yc lopropyl]c a rb onyl]a mi no]h e pt-2-e noa te 13C3,2H3,15N]-Cilastatin sodium 81129-83-1 C16H25N2NaO5S C16H26N2NaO5S Miscellaneous Enzyme APIs