Neurokinin Receptor

抑制剂选择性比较

Neurokinin Receptor产品

目录号 产品描述 文献引用 实验数据
S1189

Aprepitant

Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂,IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平,包括 G-CSFIL-6IL-8TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。

S3038

Fosaprepitant dimeglumine salt

Fosaprepitant dimeglumine salt是一种水溶性的阿瑞匹坦(aprepitant)磷酰基前体药物,是一种NK1拮抗剂。

S5476

Rolapitant

Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.

S0772New

L-732138

L-732138 is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor with IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732133 reduces hyperalgesia and has antitumor activity.

S4654

Netupitant

Netupitant (CID6451149) 是一种选择性的神经激肽1(NK1)受体拮抗剂,具有潜在的止吐剂活性。

目录号 产品描述 文献引用 实验数据
S1189

Aprepitant

Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂,IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平,包括 G-CSFIL-6IL-8TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。

S3038

Fosaprepitant dimeglumine salt

Fosaprepitant dimeglumine salt是一种水溶性的阿瑞匹坦(aprepitant)磷酰基前体药物,是一种NK1拮抗剂。

S5476

Rolapitant

Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.

S0772New

L-732138

L-732138 is a selective, potent and competitive antagonist of neurokinin-1 (NK-1) receptor with IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732133 reduces hyperalgesia and has antitumor activity.

S4654

Netupitant

Netupitant (CID6451149) 是一种选择性的神经激肽1(NK1)受体拮抗剂,具有潜在的止吐剂活性。