Neurokinin Receptor

抑制剂选择性比较

Neurokinin Receptor产品

所有产品 Neurokinin Receptor拮抗剂(5)

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-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^New	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。	Nat Commun, 2019, 10(1):17

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-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^New	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。	Nat Commun, 2019, 10(1):17