Vaborbactam

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种丝氨酸 β-内酰胺酶抑制剂，可显着恢复碳青霉烯类药物对 KPC 生产菌株的活性。

A serine β-lactamase inhibitor that notably restores the activity of carbapenems against KPC-producing strains; restores meropenem activity for 72.7 to 98.1% of CPE isolates at ≤2 ug/ml; showes no antibacterial activity alone (MICs, >64 ug/ml).Bacterial Infection Approved.

Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes. Vaborbactam restores SM 7338 activity for 72.7 to 98.1% of CPE isolates at ≤2 μg/mL, and maximum potentiation is achieved with fixed concentrations of ≥8 μg/mL of the inhibitor (≥96.5% of isolates are inhibited at ≤2 μg/mL of SM 7338-vaborbactam). SM 7338-vaborbactam with a fixed concentration of 8 μg/mL of the inhibitor (MIC50, ≤0.06 μg/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated SM 7338 MICs at ≤1 μg/mL. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase.

Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects.

RPX-7009

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

1360457-46-0

297.1351

C12H16BNO5S

>98% (HPLC)

DMSO: 10 mM

O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1

1,2-Oxaborinane-6-acetic acid, 2-hydroxy-3-[[2-(2-thienyl)acetyl]amino]-, (3R,6S)-

(-20℃)

With Ice Pack

≥ 2 years