Neurokinin Receptor

抑制剂选择性比较

特异性亚型抑制剂

NK1R Selective

Neurokinin Receptor产品

所有产品(5) Neurokinin Receptor拮抗剂(5)

目录号	产品描述	文献引用	实验数据
S1189	Aprepitant (MK-0869) 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-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。	Nat Commun, 2020, 29;11(1):2673 Neuron, 2019, 103(3):432-444 Cell Syst, 2019, 8(2):97-108	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S3038	Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517)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.
S0772	L-732138 L-732138 (L-732,138) 是一种有效的、选择性的 neurokinin-1 (NK-1) receptor/substance P (SP) receptor 的竞争性拮抗剂。L-732138 可在CHO细胞中抑制¹²⁵I-SP与稳定表达的人类NK-1受体的结合，其IC50值为2.3 nM。
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。	Nat Commun, 2019, 10(1):17

目录号	产品描述	文献引用	实验数据
S1189	Aprepitant (MK-0869) 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-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。	Nat Commun, 2020, 29;11(1):2673 Neuron, 2019, 103(3):432-444 Cell Syst, 2019, 8(2):97-108	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S3038	Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517)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.
S0772	L-732138 L-732138 (L-732,138) 是一种有效的、选择性的 neurokinin-1 (NK-1) receptor/substance P (SP) receptor 的竞争性拮抗剂。L-732138 可在CHO细胞中抑制¹²⁵I-SP与稳定表达的人类NK-1受体的结合，其IC50值为2.3 nM。
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。	Nat Commun, 2019, 10(1):17