GS-9822|HIV integrase inhibitor

Cas No.:	2219362-41-9
Chemical Name:	(S)-2-(tert-butoxy)-2-(7-(4-chlorophenyl)-5-methyl-2-(1-methyl-3-(1-(oxetan-3-yl)piperidin-4-yl)-1H-indazol-5-yl)benzo[d]thiazol-6-yl)acetic acid
Synonyms:	GS-9822,GS 9822,GS9822
SMILES:	C(O)(=O)[C@H](OC(C)(C)C)C1=C(C)C=C2C(=C1C1=CC=C(Cl)C=C1)SC(C1C=CC3=C(C=1)C(C1CCN(C4COC4)CC1)=NN3C)=N2
Formula:	C₃₆H₃₉ClN₄O₄S
M.Wt:	659.242
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GS-9822 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 3 nM.GS-9822 retains potency against mutant viruses resistant to other classes of antiretroviral agents, including protease and strand transfer integrase inhibitors.GS-9822 induces a shift in CCD helix that appears to be a result of trying to accommodate the oxetanyl piperidine moiety with shift induced by T174I mutation.Projected once-daily oral dosing makes GS-9822 suitable for combination with other ARVs.A unique and difficult-to-monitor urothelial toxicity observed in cynomolgus monkeys poses a formidable challenge for further development of GS-9822.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47607	Antiviral agent 9	Antiviral agent 9 reaches a single-digit picomolar EC50 value (0.006 nM) against HIV-1 and nearly 300-fold higher selectivity index (SI) compared to tenofovir alafenamide fumarate (TAF).
DC47606	Melliferone	Melliferone is a triterpenoid found in Brazilian propolis.
DC47605	HIV-1 inhibitor-9	HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
DC47603	Tenofovir-C3-O-C15-CF3 ammonium	Tenofovir-C3-O-C15-CF3 (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
DC47602	Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium	Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
DC47601	PMEDAP	PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality.
DC47594	Bictegravir Sodium	Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM.
DC47348	IQP-0528	IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM.
DC46814	APJ receptor agonist 1	APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
DC46427	HIV-1 inhibitor-8	HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.