| Bioactivity | 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[1][2]. |
| Invitro | ACT-660602 shows selectivity to CXCR3 over hERG, with IC50s of 18 μM (hERG)[1].ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability[1]. 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[1]. Cell Migration Assay [1] Cell Line: |
| In Vivo | ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM)[1].ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury[1].Range for Pharmacokinetics of ACT-660602[1]Animal |
| Name | ACT-660602 |
| CAS | 1646267-59-5 |
| Formula | C20H20F6N8OS |
| Molar Mass | 534.48 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. Meyer EA, et al. Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases. J Med Chem. 2022 Aug 10. [2]. Caroff Eva, et al. Preparation of piperazinyltriazolylethanone derivatives for use as CXCR3 receptor modulators: World Intellectual Property Organization, WO2015011099. 2015-01-29. |
ACT-660602
CAS: 1646267-59-5 F: C20H20F6N8OS W: 534.48
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibit
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