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CAS No. : 1646267-59-5
MCE 国际站:ACT-660602
产品活性:ACT-660602 是一种具有口服活性的趋化因子受体 CXCR3 拮抗剂, IC50 为 204 nM。ACT-660602 抑制 T 细胞迁移,并在体内急性肺损伤模型中表现出显著作用。ACT-660602 可用于自身免疫性疾病的研究。
研究领域:GPCR/G Protein | Immunology/Inflammation
作用靶点:CXCR
In Vitro: ACT-660602 shows selectivity to CXCR3 over hERG, with IC50s of 18 μM (hERG).
ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability.
ACT-660602 (5, 20, 100 or 500 nM) displays an non-competitive binding mode to CXCL10 and CXCL11 in different concentration, with more stable IC50s.
In Vivo: ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM).
ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury.
Range for Pharmacokinetics of ACT-660602
Animal | Route | Dose (range) (mg/kg) | Cmax (range) (ng/mL) | Tmax (range) (h) | AUC (range) (ng•h/mL) | F (%) | CL (range) (mL/min/kg) | Vss (range) (L/kg) | T1/2 (range) (h) |
Dog | p.o. | 2 | 1380 | 1 | 20000 | 8 | 1.3 | 1.7 | 14.5 |
| i.v. | 0.5 | 1300-1450 | 0.5-2.0 | 10400-32000 | / | 0.6-3.0 | 1.6-1.7 | 6.3- |
Rat | p.o. | 2 | 1520 | 0.5 | 14000 | 80 | 1.9 | 1.1 | 7.1 |
| i.v. | 0.5 | 1250-1860 | 0.5-1.0 | 11600-15641 | / | 1.9-1.9 | 0.9-1.3 | 5.7-8.8 |
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Small Molecule Immuno-Oncology Compound Library | Orally Active Compound Library | Chemokine Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Nicotinamide N-oxide | SX-517 | AMG 487 (S-enantiomer) | TC14012 | CTCE-9908 | CXCR2 antagonist 3 | Kynurenic acid-d5 | (R,R)-CXCR2-IN-2 | IT1t dihydrochloride | NUCC-390 | Ac-Pro-Gly-Pro-OH | Vimnerixin | NBI-74330 | CXCR4 antagonist 9 | Quetmolimab | PS372424 hydrochloride | SCH 546738 | vMIP-II (1-21) | CXCR2-IN-1 | Mavorixafor | Reparixin L-lysine salt | VUF11207 fumarate | NoxaBH3 | Kynurenic acid | CXCR4 antagonist 2 | Balixafortide | Plerixafor octahydrochloride | Ladarixin
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