CCR5 antagonist 1

CCR5 antagonist 1, derived from WO 2004054974 A2, is a CCR5 antagonist that inhibits HIV replication.

Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.

Ancriviroc (SCH-351125) is an oxime-piperidine compound with strong antiretroviral activity and an orally bioavailable small molecule chemokine receptor CCR5 antagonist (Kd value 9.27nM) that enters HIV-1 through the CCR5 co-receptor and is used to study HIV-1.

INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.

Vicriviroc maleate (SCH-417690 (maleate))(Sch-417690) is a piperazine-based CCR5 receptor antagonist with activity against human immunodeficiency virus. The IC50 value is 0.91 nM in clinical development for the treatment of HIV-1.

Cenicriviroc Mesylate is a dual CCR2 CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with a Ki of 1 nM for human CCR1, exhibiting 250-fold selectivity over CCR2, CCR5, and CXCR4.

B07 hydrochloride is a CCR5 antagonist-based inhibitor of HIV-1 entry.

Nifeviroc (TD-0232) is an orally active CCR5 antagonist used in the study of HIV-1 infection.

PF-232798 is a second generation oral CCR5 antagonist with potent broad-spectrum anti-HIV-1 activity.

AMD-3451 free base is a dual CCR5 CXCR4 antagonist which may be useful in the treatment of a wide variety of R5, R5 X4, and X4 strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2. AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction.

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

Met-RANTES (human), a partial antagonist of CCR5, diminishes the infiltration of blood monocytes into the liver [1].