GSK-729|Bacterial Inhitibor&Antagonist&Agonist|DC Chemicals

Cas No.:	1260243-45-5
Chemical Name:	(5R,7S)-5-(4-ethylphenyl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxylic acid
Synonyms:	GSK 729;GSK729
Formula:	C₁₆H₁₆F₃N₃O₂
M.Wt:	339.318
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, small molecule inhibitor of Mycobacterium tuberculosis enoyl-coenzyme A (CoA) hydratase EchA6 with IC50 of 1.8 uM, but not the MmpL3; selectively pulls down EchA6 in a stereospecific manner in M. bovis BCG extracts, competes with CoA-binding, suppresses mycolic acid synthesis, and are bactericidal in mouse model of chronic tuberculosis infection.

MSDS

COA

LOT NO.	DOWNLOAD
2018-0101

Cat. No.	Product name	Field of application
DC72935	JSF-2414	JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA.
DC72568	Cymal-6	Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) is a potent TEM-1 beta-lactamase inhibitor with an Ki value of 40.05 µM. Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) can be used as glycosidic surfactant.
DC72280	PNU-101603	PNU-101603 is a metabolite of Sutezolid. PNU-101603 has excellent activity against Mycobacterium tuberculosis (MTB).
DC72144	TH-Z145	TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM).
DC72008	UNC10201652	UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
DC71706	BPH-1086	BPH-1086 (compound 10) is an IspH inhibitor, IspH domain fused with ribosomal protein S1 (RPS1) can bind to mRNA or form part of the bacterial ribosome.
DC71474	VP-4604	VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%.
DC71466	EDA-DA	EDA-DA is an unnatural dipeptide building block (an ethynyl-D-alanine and a D-alanine). It incorporates a biorthogonal alkyne group into peptidoglycan (PG) through MurF in the cytoplasmic pathway, which enables selective labeling via a click-chemistry reaction. EDA-DA allows labeling of PG in Gram-positive (B. subtilis), Gram-negative (E. coli and C. trachomatis), Mycobacterium (M. smegmatis) and moss plastids (P. patens) with azide modified fluorescent dyes such as Alexa Fluor 488.
DC71463	WX-081	WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity.
DC70908	Xeruborbactam	Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor, inhibits class A extended-spectrum beta-lactamases with IC50 of 1-3 nM, carbapenemases such as KPC (IC50, 2.9 nM), class C P99 (IC50, 22 nM).QPX7728 displays a remarkably broad spectrum of inhibition, including class B and class D enzymes.QPX7728 is also a potent inhibitor of class D carbapenemases such as OXA-48 from Enterobacteriaceae and OXA enzymes from Acinetobacter baumannii (OXA-23/24/58, IC50 range, 1 to 2 nM) as well as MBLs such as NDM-1 (IC50, 55 ± 25 nM), VIM-1 (IC50, 14 ± 4 nM), and IMP-1 (IC50, 610 ± 70 nM).QPX7728 restored the potency of meropenem against carbapenem-resistant Enterobacterales (CRE), with the meropenem MIC90 decreasing from >64 μg/ml to 0.5 μg/ml for QPX7728 (8 μg/ml).