191672-52-3

191672-52-3 structure
191672-52-3 structure
  • Name: CS-003 Free base
  • Chemical Name: CS-003 Free base
  • CAS Number: 191672-52-3
  • Molecular Formula: C34H38Cl2N2O6S
  • Molecular Weight: 673.65
  • Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
  • Create Date: 2019-09-07 11:57:19
  • Modify Date: 2024-01-12 10:43:50
  • CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.

Name CS-003 Free base
Description CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
Related Catalog
Target

NK1:2.3 nM (Ki)

NK2:0.54 nM (Ki)

NK3:0.74 nM (Ki)

In Vitro CS-003 (0.01-10 μM; 24 hours) inhibits NK1, NK2 or NK3 induced inositol phosphate formation in a concentration-dependent manner with pA2 values of 8.7, 9.4 and 9.5 μM, respectively[1].
In Vivo CS-003 (intravenous injection; 0.01-3.0 mg/kg; 5 min before neurokinin A/B/C injection) inhibits substance P-induced tracheal vascular hyperpermeability, neurokinin A- and neurokinin B-induced bronchoconstriction with ID50 values of 0.13, 0.040 and 0.063 mg/kg, respectively[1].
References

[1]. Tsuchida H, et al. Novel triple neurokinin receptor antagonist CS-003 strongly inhibits neurokinin related responses. Eur J Pharmacol. 2008 May 31;586(1-3):306-12.

Molecular Formula C34H38Cl2N2O6S
Molecular Weight 673.65