产品
编 号：F746536
分子式：C20H20F6N8OS
分子量：534.48
分子式：C20H20F6N8OS
分子量：534.48
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1646267-59-5
产品详情
生物活性：
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.
体内研究：
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-660602AnimalRouteDose (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)
Dogp.o.2138012000081.31.714.5
i.v.0.51300-14500.5-2.010400-32000/0.6-3.01.6-1.76.3-
Ratp.o.215200.514000801.91.17.1
i.v.0.51250-18600.5-1.011600-15641/1.9-1.90.9-1.35.7-8.8
Animal Model:LPS-induced lung inflammation model (72 h post LPS challenge)
Dosage:30 mg/kg
Administration:Oral gavage; once daily
Result:Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.
体外研究：
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.
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.
体内研究：
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-660602AnimalRouteDose (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)
Dogp.o.2138012000081.31.714.5
i.v.0.51300-14500.5-2.010400-32000/0.6-3.01.6-1.76.3-
Ratp.o.215200.514000801.91.17.1
i.v.0.51250-18600.5-1.011600-15641/1.9-1.90.9-1.35.7-8.8
Animal Model:LPS-induced lung inflammation model (72 h post LPS challenge)
Dosage:30 mg/kg
Administration:Oral gavage; once daily
Result:Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备