阿瑞匹坦 T1743

Product Introduction
Bioactivity


英文名: Aprepitant

描述: Aprepitant (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。

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 12 mg/mL (22.5 mM)
DMSO : 18.33 mg/mL (34.3 mM)


关键字: Antibiotic | Human immunodeficiency virus | Bacterial | Tachykinin receptor | L754030 | Neurokinin Receptor | HIV | L 754030 | Inhibitor | MK 0869 | NK receptor | inhibit | Aprepitant | MK 869 | MK869 | MK0869

相关产品: DRB | LJ-001 | HIV-1 protease-IN-7 | Pirmitegravir | 5-Hydroxy-7,8-dimethoxyflavanone | PMEDAP | HIV-1 Nef-IN-1 | Ditiocarb sodium | Aristolactam BII | DENV-IN-5

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Highly Selective Inhibitor Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途