Published date: 2021-05-13 09:40:33
CAS number: 1436861-97-0
Name: Zidebactam
Price:
￥Inquiry/100mg
￥Inquiry/1g
Purity: 98.0%
Stocking period: Inquiry
Stock: Inquiry
Detail Product Information:
Zidebactam and WCK 5153 are novel β-lactam enhancers that are bicyclo-acyl hydrazides (BCH), derivatives of the diazabicyclooctane (DBO) scaffold, targeted for the treatment of serious infections caused by highly drug-resistant Gram-negative pathogens. In this study, we determined the penicillin-binding protein (PBP) inhibition profiles and the antimicrobial activities of zidebactam and WCK 5153 against Pseudomonas aeruginosa, including multidrug-resistant (MDR) metallo-β-lactamase (MBL)-producing high-risk clones. MIC determinations and time-kill assays were conducted for zidebactam, WCK 5153, and antipseudomonal β-lactams using wild-type PAO1, MexAB-OprM-hyperproducing (mexR), porin-deficient (oprD), and AmpC-hyperproducing (dacB) derivatives of PAO1, and MBL-expressing clinical strains ST175 (blaVIM-2) and ST111 (blaVIM-1). Furthermore, steady-state kinetics was used to assess the inhibitory potential of these compounds against the purified VIM-2 MBL. Zidebactam and WCK 5153 showed specific PBP2 inhibition and did not inhibit VIM-2 (apparent Ki [Kiapp] > 100 μM). MICs for zidebactam and WCK 5153 ranged from 2 to 32 μg/ml (amdinocillin MICs > 32 μg/ml). Time-kill assays revealed bactericidal activity of zidebactam and WCK 5153. LIVE-DEAD staining further supported the bactericidal activity of both compounds, showing spheroplast formation. Fixed concentrations (4 or 8 μg/ml) of zidebactam and WCK 5153 restored susceptibility to all of the tested β-lactams for each of the P. aeruginosa mutant strains. Likewise, antipseudomonal β-lactams (CLSI breakpoints), in combination with 4 or 8 μg/ml of zidebactam or WCK 5153, resulted in enhanced killing. Certain combinations determined full bacterial eradication, even with MDR MBL-producing high-risk clones. β-Lactam–WCK enhancer combinations represent a promising β-lactam “enhancer-based” approach to treat MDR P. aeruginosa infections, bypassing the need for MBL inhibition.
Name: Hebei We Together Medical Technology Co., Ltd.
Chemsrc Level: Unverified
Product #: 14
Tel: 13180081292
Address: China,Hebei Province,Shijiazhuang city,High-tech District,Taishan Street No. 219-19, Second floor
Area: China(Mainland)
Contact: Richard Wang
Contact Phone #: 13180081292
Email: wetogethermeditech@163.com
Website: http://www.wetogethermed.com
Annual Trade Volume: 100w
Foreign Trade % of Salers:
Major partners:
Detail
introduction:
Hebei We-Together Meditech Co., Ltd. focus on Antibiotic enhancement agent (Antibiotic Enhancer) especially for β-lactamase inhibitor pipeline drugs as the business line, provides Avibactam, Relebactam, Zidebactam, Vaborbactam, WCK-5153, etc Series of β-lactamase inhibitors intermediates, impurities, R & D production, technical services and technology transfer ,etc.
Name: Shanghai Nianxing Industrial Co., Ltd
Area: China
Price:
￥Inquiry/100mg
￥Inquiry/1g
Contact: Yang
Product Detail: Zidebactam
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