HIV Infection|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Human immunodeficiency virus (HIV) is an infection that attacks the body’s immune system, specifically the white blood cells called CD4 cells. HIV destroys these CD4 cells, weakening a person’s immunity against infections such as tuberculosis and some cancers.

WHO recommends that every person who may be at risk of HIV should access testing. People diagnosed with HIV should be offered and linked to antiretroviral treatment as soon as possible following diagnosis. If taken consistently, this treatment also prevents HIV transmission to others.

If the person’s CD4 cell count falls below 200, their immunity is severely compromised, leaving them more susceptible to infections. Someone with a CD4 count below 200 is described as having AIDS (acquired immunodeficiency syndrome).

Cat. No.	Product Name	CAS No.	Information
H9583	Pirmitegravir	2245231-10-9	Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
H7563	Go 6976	136194-77-9	A potent, selective protein kinase C (PKC) inhibitor that selectively inhibits PKCα and PKCβ1 with IC50 of 2.3 and 6.2 nM, respectively; shows no effect on the kinase activity of PKCδ, -ε and -ζ (IC50>3 uM); also inhibits JAK2, FLT3 and mutant FLT3 with significant activity in primary acute myeloid leukaemia cells; inhibits HIV-1 proviral induction from latent/low-level-producing infectious states, inhibits signalling, survival and proliferation in cells expressing the leukaemia-associated TEL-JAK2 fusion protein and the MPD-associated JAK2 V617F mutant.
H5047	Cobicistat	1004316-88-4	A pharmacoenhancer that acts as potent and selective inhibitor of human CYP3A with IC50 of 30-285 nM; more selective than RTV with much reduced inhibitory activity toward CYP2D6, CYP2C8, and CYP2C9.
H3212	Vicriviroc maleate	599179-03-0	A potent, highly selective, and orally bioavailable CCR5 antagonist with Ki of 2.5 nM; display no affinity for muscarinic receptors (Ki>10 uM); inhibits HIV-1 entry into U-80 cells with IC50 of 0.8 nM, inhibits HIV-1 clinical isolates in PBMC with IC90 of 1-10 nM; exhibits excellent receptor selectivity and oral bioavailability in rats and monkeys.
H3210	TAK-220	333994-00-6	A potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM; shows no affinity for CCR1, CCR2b, CCR3, CCR4, or CCR7; inhibits the replication of 6 CCR5-using (R5) HIV-1 clinical isolates in peripheral blood mononuclear cells (PBMCs) with mean EC90 of 13 nM; selectively inhibits R5 HIV-1 replication by interfering with coreceptor-mediated entry of the virus into host cells; exhibits a good pharmacokinetic profile in monkeys.
H3194	POL3026	918660-21-6	A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.2 nM in Ca2+ flux assay; shows excellent plasma stability, high selectivity for CXCR4, favorable pharmacokinetic properties in vivo, has the potential to become a therapeutic compound for application in the treatment of HIV infections (as an entry inhibitor), cancer (for angiogenesis suppression and inhibition of metastasis), inflammation, and in stem cell transplant therapy.
H3190	PF-232798	849753-15-7	PF-232798 (PF-00232798) is a potent CCR5 antagonist with IC50 of 12 uM); demonstrates antiviral activity against HIV BaL in PBMCs with IC50 of 2.0 nM.
H3167	INCB9471	869769-98-2	A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs; inhibits CCR5-mediated signaling events such as intracellular calcium mobilization, ERK phosphorylation, and CCR5 receptor internalization with IC50 values of 16, 3, and 1.5 nM, respectively; demonstrates anti-HIV-1 activity against R5 HIV-1 strains representing the major clades including A, B, C, D, E, F, G, and J with mean IC50 of 9 nM in PBMCs; also is a potent inhibitor of mutant HIV-1 variants that are resistant to other drugs including NRTIs, NNRTIs, PIs, and the fusion inhibitor T20.
H3107	Aplaviroc hydrochloride	461023-63-2	Aplaviroc (GSK-873140;GW 873140;AK-602;ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6; blocks the calcium response effects of CCR5 activation by CCL5, and potently blocks in vitro the infection of R5-tropic HIV-1 (R5-HIV-1) at subnanomolar IC50. 3
H3106	Aplaviroc	461443-59-4	Aplaviroc (GSK-873140;GW 873140;AK-602;ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6; blocks the calcium response effects of CCR5 activation by CCL5, and potently blocks in vitro the infection of R5-tropic HIV-1 (R5-HIV-1) at subnanomolar IC50.

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