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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.
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 .
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.
CB-0821 is a high affinity CCR5 inhibitor with a Ki of 0.04 nM. CB-0821 binds efficiently to the hydrophobic pocket of the CCR5 protein, to inhibit the interactions between viral protein and CCR5, thereby inhibiting viral entry. CB-0821 has the potential for anti-HIV research .
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 .
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 .
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 .
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.
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells . Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells .
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.
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 .
Met-RANTES (human) is the antagonist for CCR1 and CCR5. Met-RANTES (human) inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
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).
Met-RANTES (human) acetate is the acetate form of Met-RANTES (human) (HY-P4191). Met-RANTES (human) acetate is the antagonist for CCR1 and CCR5. Met-RANTES (human) acetate inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) acetate reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
Vicriviroc (SCH 417690) is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer .
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 .
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 .
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 .
Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
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 .
Met-RANTES (human) is the antagonist for CCR1 and CCR5. Met-RANTES (human) inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
Met-RANTES (human) acetate is the acetate form of Met-RANTES (human) (HY-P4191). Met-RANTES (human) acetate is the antagonist for CCR1 and CCR5. Met-RANTES (human) acetate inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) acetate reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
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 .
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 .
Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
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 (HEK293, Flag, His, Strep) is the recombinant human-derived CCR5 protein, expressed by HEK293 Cell-free , with N-Flag, C-His, C-Strep labeled tag.
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].
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.
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