GSK-656

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

GSK-656 (GSK-3036656, GSK656) 是一种有效、高选择性、口服生物可利用的 Mtb Leucyl-tRNA 合成酶 (LeuRS)，IC50 为 0.2 uM。

GSK-656 (GSK-3036656, GSK656)?is a potent, highly selective,orally bioavailable Mtb Leucyl-tRNA synthetase (LeuRS) with IC50 of 0.2 uM; displays no significant activity for human mitochondrial LeuRS and human cytoplasmic LeuRS (IC50>100 uM); shows potent antitubercular activity (Mtb H37Rv IC50=0.08 uM) in vitro; exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models.Bacterial Infection.Phase 1 Clinical.

Ganfeborole hydrochloride is highly selective inhibitor for Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM, and shows IC50s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. Ganfeborole hydrochloride exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. Ganfeborole hydrochloride also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis.

Ganfeborole hydrochloride shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg.

GSK656 | GSK 656 | GSK3036656 | GSK-3036656

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

2131798-13-3

293.935

C10H14BCl2NO4

>98% (HPLC)

DMSO : 67.5 mg/mL 229.64 mM

B1(C2=C(C=CC(=C2C(O1)CN)Cl)OCCO)O.Cl

(S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c]-[1,2]oxaborol-1(3H)-ol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years