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Aprepitant 是选择性和高亲和力的神经激肽1受体拮抗剂,Kd 值为86 pM。
Aprepitant 是选择性和高亲和力的神经激肽1受体拮抗剂,Kd 值为86 pM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 233 | 现货 | |
5 mg | ¥ 533 | 现货 | |
10 mg | ¥ 756 | 现货 | |
25 mg | ¥ 1,290 | 现货 | |
50 mg | ¥ 1,920 | 现货 | |
100 mg | ¥ 2,860 | 现货 | |
200 mg | ¥ 4,150 | 现货 | |
500 mg | ¥ 6,490 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 597 | 现货 |
产品描述 | Aprepitant is a Substance P/Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer. |
靶点活性 | NK1 receptor:0.1 nM |
体外活性 | 在疼痛冲动从外周受体到CNS 的传感中,Aprepitant起关键作用,并参与对压力的各种行为及神经化学和心血管的反应.Aprepitant可穿透血脑屏障并与大脑中NK-1受体结合.Aprepitant可抑制化疗引起的细胞毒性,如顺铂(阻断P物质)诱发的急性和延迟性呕吐.Aprepitant(3 mg/kg,i.v.或p.o.)可抑制顺铂(10 mg/kg,i.v.)引起的呕吐.Aprepitant(0.1 mg/kg,i.v.)与地塞米松(20 mg/kg,i.v.)或5–HT3 受体拮抗剂恩丹西酮(0.1 mg/kg,i.v.)联用可加强止吐效果.在雪貂急性迟缓性呕吐模型中,顺铂(5 mg/kg,i.p.)给药后恶心并呕吐的回应记录为72 h.Aprepitant(4-16 mg/kg,p.o.)预处理可剂量依赖性地抑制顺铂引起的呕吐.Aprepitant(2-4 mg/kg/day,p.o.)完全抑制了所有给药雪貂的恶心和呕吐症状.通过注射顺铂24 h后可形成呕吐急性期,开始每天给药,顺铂注射后 24 和48 h,Aprepitant(4 mg/kg,p.o.) 抑制了75%雪貂的恶心和呕吐症状. |
体内活性 | Aprepitant对人NK1受体的选择性是人NK3受体的3000倍,比人NK2受体多出50,000倍。在使用人类和动物组织(IC50> 3 μM)进行的单胺摄取位点(NE, 5–HT, DA)计数筛选中,以及在人类单胺氧化酶A和B试验以及人类血清素5–HT1A, 5–HT2A, 5–HT2c, 5–HT3, 5–HT5, 5–HT6,和5–HT7 受体(IC50>3 μM)中,Aprepitant均是无活性的。Aprepitant与CNS和外周的NK-1受体结合而拮抗P物质。CHO或 COS 细胞中hNK1受体上50%的P物质会被Aprepitant(0.1 nM)取代。在放射性配体结合试验中,在放射性配体结合筛选的PANLABS 板中,采用原生动物组织,Aprepitant抑制大鼠颌下腺中[3H]P物质与天然NK1受体结合;经检查PANLABS筛选,Aprepitant与其他任何原生动物G蛋白耦合的受体或离子通道均无明显的相互作用。 |
细胞实验 | Aprepitant is dissolved in DMSO. The inhibitory effect of aprepitant on metabolic activity of Nalm-6 cells is assessed by uptake of thiazolyl blue tetrazolium bromide (MTT) by viable cells. Cells are plated onto 96-well plates at a density of 5000 cells/well. After treatment with aprepitant at 5, 10, 15, 20 and 30 μM for 24, 36 and 48 h, the cells are further incubated with 100 μL of MTT (0.5 mg/mL) at 37°C for 3 h. Untreated cells are defined as the control group. Following solubilization of precipitated formazan with 100 μL of DMSO, the optical densitometry is measured with an ELISA reader at a wavelength of 578 nm. |
别名 | 阿瑞匹坦, MK-869, MK-0869, L-754030, Aprepitant` |
分子量 | 534.43 |
分子式 | C23H21F7N4O3 |
CAS No. | 170729-80-3 |
Smiles | C(N1[C@H]([C@@H](O[C@H](C)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)OCC1)C3=CC=C(F)C=C3)C4=NNC(=O)N4 |
密度 | 1.51 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | Ethanol: 12 mg/mL (22.5 mM) DMSO: 18.33 mg/mL (34.3 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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