Cenicriviroc

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cenicriviroc 是一种口服活性的 CCR2/CCR5 双重拮抗剂。它还可以抑制 HIV-1 和 HIV-2，并具有有效的抗感染和抗炎活性。

Cenicriviroc is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity.(In Vitro):Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC50 for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC50 at >1000 nM, and MPI at 33% and 4%, respectively.(In Vivo):Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight.

Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC50?for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC50 at >1000 nM, and MPI at 33% and 4%, respectively.

Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight.

TAK-652 | TBR-652

Autophagy

CCR

CCR2| CCR5| HIV-1| HIV-2

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497223-25-3

696.94

C42H52N4O4

>98% (HPLC)

DMSO:120 mg/mL (172.19 mM)

CCCCOCCOC1=CC=C(C=C1)C2=CC/3=C(C=C2)N(CCC/C(=C3)/C(=O)NC4=CC=C(C=C4)[S@@](=O)CC5=CN=CN5CCC)CC(C)C

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(-20℃)

With Ice Pack

≥ 2 years