CS-003 Free base

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.

产品编号 T10892Cas号 191672-52-3

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CS-003 Free base

产品编号 T10892Cas号 191672-52-3

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规格	价格	库存
25 mg	¥ 18,300	10-14周
50 mg	¥ 24,300	10-14周
100 mg	¥ 31,500	10-14周

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生物活性

产品描述	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.
靶点活性	NK1:2.3 nM (ki), NK2:0.54 nM (ki), NK3:0.74 nM (ki)
体外活性	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.
体内活性	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.

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