ccr1

CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).

CCR1 5 8 activator 1 is a cytoplasmic phospholipase A inhibitor with antifungal activity.

CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 (CCR1) antagonist with an IC50 of 4 nM [1].

CCR1 antagonist 9 is an effective and selective CCR1 antagonist (IC50: 6.8 nM in calcium flux assay).

MLN-3897 TFA is a potent CCR1 antagonist that inhibits the binding of 125I-MIP-1α to THP-1 cell membranes.

CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with IC50 values of 0.03 μM for hCCR1, 0.58 μM for mCCR1, and 0.32 μM for rCCR1. This compound is useful for studying rheumatoid arthritis and other related inflammatory diseases.

CCR1 antagonist12 (Compound 12) is an antagonist of CCR1, exhibiting an IC50 of 3 nM against human CCR1. It inhibits the chemotaxis through pores induced by CCL3, with an IC50 of 0.009 µM. Additionally, CCR1 antagonist12 demonstrates favorable pharmacokinetic properties in a rat model.

CCX354 (CCR1 antagonist 1) is a potent small molecule CCR1 antagonist with anti-inflammatory activity for the treatment of rheumatoid arthritis.

BMS-817399 is an orally active antagonist of CCR1 with IC50s of binding affinity and chemotaxis inhibition potencies and can be used in studies about rheumatoid arthritis.

MLN-3897 (CCR1 antagonist 10) is an orally active antagonist of CCR1 with a Ki of 2.3 nM for 125I-MIP-1α binding to THP-1 cell membranes. MLN-3897 inhibits Akt signaling and MM cell survival and proliferation.

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

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.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

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.

YM022 is a highly effective and selective gastrin cholecystokinin (CCK)-B receptor antagonist. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively.

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.

chemokine CCR1 and CCR3 receptor antagonist

BMS-457 is a potent, CCR1-selective antagonist.

AZD-4818 (CCR1 antagonist) is a chemokine CCR1 antagonist for the treatment of chronic obstructive pulmonary disease.

CP 481715 is an effective selective CCR1 antagonist with potential therapeutic significance for inflammatory diseases.

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells with IC50 values of 5.4 nM and 3.4 nM, respectively. Vercirnon sodium demonstrates high selectivity, showing IC50 values exceeding 10 µM for CCR1-12 and CX3CR1-7 receptors. It also inhibits CCL25-directed chemotaxis in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively.