| Description | CS-003 free base (CS-003) is a triple tachykinin receptor antagonist with high affinity for human (neurokinin) NK1, NK2 and NK3 receptors, with Ki values of 2.3 nM and 0.54 nM, respectively And 0.74 nM. CS-003 free base (CS-003) has therapeutic effects on neurokinin-related respiratory diseases. |
| In vitro | CS-003 (0.01-10 μM; 24 hours) inhibited inositol phosphate formation induced by NK1, NK2 or NK3 in a concentration-dependent manner, with pA2 values of 8.7, 9.4 and 9.5 μM, respectively. |
| In vivo | CS-003 (intravenous injection; 0.01-3.0 mg / kg; neurokinin A / B / C 5 minutes before injection) inhibits substance P-induced increase in tracheal vascular permeability, induced by neurokinin A and neurokinin B The bronchi contracted and the ID50 values were 0.13, 0.040 and 0.063 mg / kg, respectively. |
| Target activity | NK1:2.3 nM (ki), NK2:0.54 nM (ki), NK3:0.74 nM (ki) |
| molecular weight | 673.65 |
| Molecular formula | C34H38Cl2N2O6S |
| CAS | 191672-52-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 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. |