[CAS NO. 1436861-97-0] Zidebactam

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PRODUCTS SPECIFICATIONS [1436861-97-0]

Catalog

HY-120859

Brand

MCE

CAS

1436861-97-0

DESCRIPTION [1436861-97-0]

Overview

MDL	-
Molecular Weight	391.40
Molecular Formula	C13H21N5O7S
SMILES	O=C([C@@H]1CCCNC1)NNC([C@@H]2CC[C@@H]3C[N@]2C(N3OS(=O)(O)=O)=O)=O

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

Zidebactam (WCK-5107) is a potent β-lactamase inhibitor ^[1] . Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC ₅₀ of 0.26 μg/mL ^[2] .

IC50 & Target

IC50: 0.26 μg/mL ( P. aeruginosa PAO1 PBP2) ^[2]

In Vitro

Zidebactam (WCK-5107) inhibits WT Enterobacteriaceae with a MIC ₅₀ of 0.25 mg/L. Zidebactam alone exhibits variable activity when tested against E. coli (MIC _50/90 0.12/0.12 mg/L) and Enterobacter spp. (MIC _50/90 0.12/0.25 mg/L) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02532140	Wockhardt\|Quintiles, Inc.	Healthy	August 2015	Phase 1
NCT02674347	Wockhardt\|Quintiles, Inc.	Healthy Subjects	February 2016	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 638.73 mM ; Need ultrasonic)

H ₂ O : 50 mg/mL ( 127.75 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5549 mL	12.7747 mL	25.5493 mL
5 mM	0.5110 mL	2.5549 mL	5.1099 mL
10 mM	0.2555 mL	1.2775 mL	2.5549 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (255.49 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.98 mg/mL (5.06 mM); Clear solution

* All of the co-solvents are available by MCE.