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Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂,Ki 值为0.66 nM。
Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂,Ki 值为0.66 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 358 | 现货 | |
2 mg | ¥ 518 | 现货 | |
5 mg | ¥ 859 | 现货 | |
10 mg | ¥ 1,380 | 现货 | |
25 mg | ¥ 2,190 | 现货 | |
50 mg | ¥ 3,630 | 现货 | |
100 mg | ¥ 5,230 | 现货 | |
500 mg | ¥ 10,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,020 | 现货 |
产品描述 | Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. |
靶点活性 | NK1:0.66 nM. (Ki) |
体外活性 | Rolapitant对人类NK1受体具有高亲和力,Ki值为0.66 nM,且对人类NK2和NK3亚型的选择性超过1000倍。Rolapitant对人类、豚鼠、沙鼠和猴子的NK1受体具有较高亲和力,相较于大鼠、小鼠和兔子的NK1受体[1]。 |
体内活性 | Rolapitant 通过静脉注射和口服给药,在最小有效剂量(MED)0.1 mg/kg 下,可逆转NK1激动剂在沙鼠中引起的脚踏动作,持续时间达24小时。在急性和延迟呕吐模型中,Rolapitant 在0.1和1 mg/kg剂量下对雪貂均有效,这与其他NK1拮抗剂的临床数据一致。抗呕吐药的临床效果与雪貂呕吐模型中的效果高度相关,暗示Rolapitant是这一适应症的有力临床候选者[1]。 |
激酶实验 | Rolapitant is made at a stock concentration of 1 mM in 100% DMSO. For most receptor binding studies, the stock solution is diluted with the final concentrations ranged from 0.1 to 3 μM. Radioligand concentrations for competition binding studies ranged from 0.5 to 1 nM. For species comparison studies, 150 pM [125I]-BHSP is incubated with varying concentrations of protein (10-50 μg) prepared from gerbil, rabbit and monkey striata, and from cells expressing cloned rat, mouse and guinea pig NK receptors[1]. |
别名 | 罗拉匹坦, 罗拉吡坦, SCH619734 |
分子量 | 500.48 |
分子式 | C25H26F6N2O2 |
CAS No. | 552292-08-7 |
Smiles | [H][C@](C)(OC[C@]1(CC[C@]2(CCC(=O)N2)CN1)c1ccccc1)c1cc(cc(c1)C(F)(F)F)C(F)(F)F |
密度 | 1.34 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 | DMSO: 55 mg/mL (109.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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