|Cat. No.||Product Name||CAS No.||Information|
BX471 is a potent, selective, non-peptide CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1; shows 10,000-fold selectivity for CCR1 compared with 28 GPCRs (); displays CCR1 ligands MIP-1α, RANTES, and MCP-3 with high affinity (Ki=1-5.5 nM), inhibits a number of CCR1-mediated effects including Ca(2+) mobilization, increase in extracellular acidification rate, CD11b expression; effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis.
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.
(S)-CCX-777 is a small-molecule partial agonist of CXCR7 (ACKR3).
(R)-CCX-777 is a small-molecule partial agonist of CXCR7 (ACKR3).
CCX-777 is a small-molecule partial agonist of CXCR7 (ACKR3).
CCX-354 (GSK-2941266, CCX354-C, CCX354) is a potent, selective, orally-available CCR1 antagonist for the treatment of inflammatory diseases such as rheumatoid arthritis (RA).
CCR1 inhibitor 19e
CCR1 inhibitor 19e is a novel potent, selective CCR1 antagonist with IC50 of 6.8 nM, inhibits CCR1chemotaxis in THP-1 cells with IC50 of 28 nM.
LIT-927 (LIT927) is the first selective, locally and orally active CXCL12 neutraligand with Ki of 267 nM for CXCL12-TR binding inhibition; displays excellent selectivity over other chemokines (CCL17, CCL22, CCL5 and CCL2), inhibits the increase in intracellular calcium concentration in EGFP-CXCR4+HEK cells in response to CXCL12 at 10 uM, has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or by CCL2 on EGFP-CCR2+HEK cells; reduces eosinophil recruitment in murine model of allergic airway hypereosinophilia.
AZ084 (AZ-084) is a potent, selective, allosteric, orally available CCR8 antagonist with Ki of 0.9 nM; demonstrates excellent selectivity in a panel of 141 kinases and receptors, also shows no binding activity at 10 uM towards any of the other chemokine receptors; demonstrates excellent selectivity, high metabolic stability in vitro and an attractive in vivo PK profile with a long half-life in rats; inhibits dendritic cell, T cell and eosinophil migration.
BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively; displays excellent selectivity against a panel of additional chemokine receptors including human CCR2, CCR4, CCR5, CCR6, CCR7, CXCR1, CXCR2, and CXCR3; suppresses colon cancer liver metastasis by blocking accumulation of immature myeloid cells in a mouse mode; ameliorates the progression of lupus nephritis in NZB/W mice; also improves survival, decreases the kidney fungal burden and protects from renal tissue injury in Candida-infected mice.
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