ACT-660602 (C09-1101-500)

ACT-660602 is an orally active antagonist of chemokine receptor ( CXCR3 ) with an IC 50 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 researchIn VitroACT-660602 shows selectivity to CXCR3 over hERG, with IC 50 s 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 IC 50 s. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Migration AssayCell Line: CD3/CD28-activated primary human T cells Concentration: 112 nM Incubation Time: 45 min Result: Inhibited cell migration.In VivoACT-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) C max (range) (ng/mL) T max (range) (h) AUC (range) (ng•h/mL) F (%) CL (range) (mL/min/kg) V ss (range) (L/kg) T 1/2 (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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:CXCR3 204 nM (IC 50 ). Specifications and Purity: 99%. Molecular Formula: C20H20F6N8OS. Molecular Weight: 534.48.