ccr5

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

Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW.

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

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.

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM. AZD-5672 inhibits hERG cardiac ion channel binding and P-gp-mediated digoxin transport with IC50s of 7.3 μM and 32 μM. AZD-5672 can be used in studies about rheumatoid arthritis.

BMS-813160 is the first dual CCR2/CCR5 antagonist to enter Clinical development for cardiovascular.

DAPTA (Adaptavir) is an inhibitor of CCR5, shows potent anti-HIV activities.

Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody with both anti-HIV and anti-tumor activity, inhibiting CCR-mediated HIV-1 virus and cancer cell metastasis in mouse tumor models. Leronlimab can be used to study HIV, non-alcoholic steatohepatitis (NASH), and breast cancer.

WAY-639418 has potential anti-inflammatory and anti-HIV activity and can be used to study CCR5-mediated inflammatory and immunomodulatory diseases.

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.

CCR5-IN-1 (compound 3ad) is an allosteric, selective inhibitor of CCR5 with an IC50 of 1.09 μM. It is applicable in research related to cardiovascular, central nervous system, immune system, and infectious diseases.

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.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

PF-0463481 succinate is a potent and orally active dual antagonist of CCR2/CCR5, exhibiting comparable human and rodent CCR2 potency with an IC50 of 20.8 nM.

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.

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.

Met-RANTES (human) acetate is the acetate salt form of Met-RANTES (human). It acts as an antagonist for CCR1 and CCR5 receptors. This compound inhibits the human chemokines MIP-1α and MIP-1β, with respective IC50 values of 5 and 2 nM. Additionally, Met-RANTES (human) acetate reduces bone destruction and alleviates adjuvant-induced arthritis (AIA) in rats.

INCB10820 is an efficient and specific dual antagonist of CCR2 and CCR5, with oral bioavailability.

GSK163929 (compound 122) is an orally active CCR5 antagonist with anti-HIV properties and demonstrates low inhibitory potency against hEGR. Administered at a dosage of 2000 mg kg day (i.v., 7 d), it shows no adverse effects in rats, and at 250 mg kg day (i.v., 7 d), it is similarly non-toxic in dogs.

CB-0821 is a high-affinity CCR5 inhibitor with a Ki of 0.04 nM. It effectively binds to the hydrophobic pocket of the CCR5 protein, hindering the interaction between viral proteins and CCR5, thereby blocking virus entry. CB-0821 holds potential for anti-HIV research.