[CAS NO. 118081-34-8] Ceftibuten dihydrate

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PRODUCTS SPECIFICATIONS [118081-34-8]

Catalog

HY-B0698A

Brand

MCE

CAS

118081-34-8

DESCRIPTION [118081-34-8]

Overview

MDL	MFCD08141796
Molecular Weight	446.46
Molecular Formula	C15H18N4O8S2
SMILES	O=C(C(N12)=CCS[C@]2([H])[C@H](NC(/C(C3=CSC(N)=N3)=C\CC(O)=O)=O)C1=O)O.O.O

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

1 Publications Citing Use of MCE

[1]SLAS Discov. 2020 Sep;25(8):895-905.

Summary

Ceftibuten (Sch-39720) dihydrate, an antibiotic , is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens ^[1] ^[2] .

In Vitro

Ceftibuten (Sch-39720) is highly active against Haemophilus influenza , Escherichia coli , Klebsiella sp., and Proteus sp. and moderately active against Serratia sp. and Streptococcus pyogenes . Ceftibuten is relatively inactive against enterococci and staphylococci and is only weakly active against Pseudomonas aeruginosa and obligate anaerobes. It is also stable in the presence of most β-lactamase-producing organisms except β Bacteroides fragilis . Ceftibuten is very active against strains of the family Enterobacteriaceae (mean MIC for 90% of strains=0.25 μg/ml) but less active against Campylobacterjejuni (mean MIC for 90% of strains=16.0 μg/ml) ^[1] .

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

In Vivo

Ceftibuten, a biologically stableβ-lactam antibiotic, has been shown to be transported by the small peptide transport system, to have relatively high affinity for the carrier and to show clear stereoselective and proton-gradient dependent transport characteristics in rat intestinal brush-border membrane vesicles ^[3] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00724256	IRCCS Burlo Garofolo	Pyelonephritis	July 2006	Phase 3
NCT05488678	Venatorx Pharmaceuticals, Inc.\|National Institute of Allergy and Infectious Diseases (NIAID)	Pharmacokinetics	October 12, 2022	Phase 1
NCT04877379	Venatorx Pharmaceuticals, Inc.\|National Institute of Allergy and Infectious Diseases (NIAID)	Healthy Subjects	June 8, 2021	Phase 1
NCT05527834	Venatorx Pharmaceuticals, Inc.\|National Institute of Allergy and Infectious Diseases (NIAID)	Pharmacokinetics	September 13, 2022	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 : 100 mg/mL ( 223.98 mM ; Need ultrasonic)

H ₂ O : 100 mg/mL ( 223.98 mM ; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2398 mL	11.1992 mL	22.3984 mL
5 mM	0.4480 mL	2.2398 mL	4.4797 mL
10 mM	0.2240 mL	1.1199 mL	2.2398 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
3.

Add each solvent one by one: PBS

Solubility: 2.26 mg/mL (5.06 mM); Clear solution; Need ultrasonic

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

References

Synonyms

5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2Z)-2-(2-amino-4-thiazolyl)-4-carboxy-1-oxo-2-buten-1-yl]amino]-8-oxo-, hydrate (1:2), (6R,7R)-

5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[2-(2-amino-4-thiazolyl)-4-carboxy-1-oxo-2-butenyl]amino]-8-oxo-, dihydrate, [6R-[6α,7β(Z)]]-

(6R,7R)-7-[[(2Z)-2-(2-Amino-4-thiazolyl)-4-carboxy-1-oxo-2-buten-1-yl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid hydrate (1:2)