Top Suppliers:I want be here
Related CAS#:
1646267-59-5 121368-75-0
1159501-31-1 1433875-14-9
1361321-96-1 1258417-54-7
1103522-45-7 1838651-58-3
1354039-86-3 1159500-34-1
2810138-34-0 218931-38-5
156189-40-1 2934621-29-9
2937046-82-5 1403605-09-3
2776206-75-6 2776206-74-5
1822425-62-6 2803467-40-3

1646267-59-5

1646267-59-5 structure
1646267-59-5 structure
  • Name: ACT-660602
  • Chemical Name: ACT-660602
  • CAS Number: 1646267-59-5
  • Molecular Formula: C20H20F6N8OS
  • Molecular Weight: 534.48
  • Catalog: Signaling Pathways GPCR/G Protein CXCR
  • Create Date: 2022-10-12 18:25:38
  • Modify Date: 2024-04-05 18:53:44
  • 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].
Name ACT-660602
Description 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].
Related Catalog
Target

CXCR3:204 nM (IC50)

In Vitro 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: CD3/CD28-activated primary human T cells Concentration: 112 nM Incubation Time: 45 min Result: Inhibited cell migration.
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 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 Animal Model: LPS-induced lung inflammation model (72 h post LPS challenge)[1] Dosage: 30 mg/kg Administration: Oral gavage; once daily Result: Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.
References

[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.
Molecular Formula C20H20F6N8OS
Molecular Weight 534.48
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.

Chemsrc provides CAS#:1646267-59-5 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 1646267-59-5 | Chemsrc address: https://m.chemsrc.com/en/baike/1719590.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved