CS-003 Free base (CS-003)是一种三速激肽受体拮抗剂，对人神经激肽 (Neurokinin) NK1，NK2 和 NK3 受体具有高亲和力，Ki 值分别为 2.3 nM，0.54 nM 和 0.74 nM。CS-003 Free base (CS-003) 对与神经激肽有关的呼吸系统疾病具有治疗功效。
CAS：191672-52-3
分子式：C34H38Cl2N2O6S
分子量：673.65
纯度：98%
存储：Store at -20°C

Background:

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. NK1|2.3 nM (Ki)|NK2|0.54 nM (Ki)|NK3|0.74 nM (Ki)

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].

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].

[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.