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.

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.

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.

191672-52-3

C34H38Cl2N2O6S

673.65

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years