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CCR5 antagonist 5 (compound example 11) is a CCR5 antagonist. CCR5 antagonist 5 has the potential to study inflammation and immunity and viral (such as HIV) infection .
CCR5 Human Pre-designed siRNA Set A contains three designed siRNAs for CCR5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Ccr5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ccr5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Ccr5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ccr5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor .
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity .
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
RPR103611, the betulinic acid derivative, is a potent HIV-1 entry inhibitor with IC50s of 80, 0.27, and 0.17 for CCR5-tropic virus YU2, CXCR4-tropic virus NL4-3 and dual tropic virus 89.6, respectively .
BMS-813160 is a potent and selective CCR2/5 dual antagonist. BMS-813160 binds with CCR2 and CCR5 with IC50s of 6.2 and 3.6 nM, respectively. BMS-813160 can be used for the research of inflammation .
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
Murabutide is a safe synthetic immunomodulator. Murabutide can reduce CD4 and CCR5 receptor expression and secrete high levels of beta-chemokines. Murabutide enhances nonspecific resistance against viral infections. Murabutide did not affect virus entry, reverse transcriptase activity or early proviral DNA formation in the cytoplasm of infected cells .
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. 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 .
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor .
CCR5 Protein, a receptor for inflammatory CC-chemokines, including CCL3/MIP-1-alpha, CCL4/MIP-1-beta, and RANTES, plays a crucial role in signal transduction by increasing intracellular calcium ion levels. It contributes to granulocytic lineage control and T-lymphocyte migration to infection sites, serving as a chemotactic receptor. Interactions with PRAF2, GRK2, ARRB1, ARRB2, and CNIH4 highlight CCR5's regulatory network complexity. Efficient ligand binding to CCL3/MIP-1alpha and CCL4/MIP-1beta requires sulfation, O-glycosylation, and sialic acid modifications. Glycosylation on Ser-6 is essential for optimal CCL4 binding. The stimulating effect on T-lymphocyte chemotaxis, observed in interaction with S100A4, emphasizes CCR5's multifaceted roles in immune responses and cellular signaling pathways. CCR5 Protein, Mouse (P. pastoris, His) is the recombinant mouse-derived CCR5 protein, expressed by P. pastoris, with N-6*His labeled tag. The total length of CCR5 Protein, Mouse (P. pastoris, His) is 92 a.a., with molecular weight of 12.6 kDa.
CCR5 Protein, a receptor for inflammatory CC-chemokines like CCL3/MIP-1-alpha, CCL4/MIP-1-beta, and RANTES, transduces signals, elevating intracellular calcium levels. It regulates granulocytic lineage and facilitates T-lymphocyte migration to infection sites. In microbial infection, CCR5 acts as a coreceptor, along with CD4, for HIV-1, emphasizing its role in the cellular response to infections. CCR5 Protein, Human (Cell-Free, His) is the recombinant human-derived CCR5 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CCR5 Protein, Human (Cell-Free, His) is 352 a.a., with molecular weight of 43.9 kDa.
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
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