HIV InSTI-1|HIV integrase strand transfer inhibitor 1

Cas No.:	1549802-58-5
Chemical Name:	(1R,2R,5S)-8'-(3-chloro-4-fluorobenzyl)-6'-hydroxy-2'-((S)-2-hydroxypropyl)-9',10'-dihydro-2'H-spiro[bicyclo[3.1.0]hexane-2,3'-imidazo[5,1-a][2,6]naphthyridine]-1',5',7'(8'H)-trione
Synonyms:	HIV integrase strand transfer inhibitor 1
SMILES:	[C@@]([H])12[C@@]([H])(C1)CC[C@@]21N(C[C@H](O)C)C(=O)C2=C3C(C(=O)N(CC4=CC=C(F)C(Cl)=C4)CC3)=C(O)C(=O)N21
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent HIV integrase strand transfer inhibitor (InSTIs) with IC50 of 8 nM in HIV replication assay; shows Mutant Fold Shift 1/1/1/1/2/4 for E92Q/Y143R/Q148R/Q148K/N155H/G140S-Q148H compared with WT enzyme, respectively; demonstrates desired virological profile and preclinical pharmacokinetic profile.

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.