Rolapitant
(Synonyms: 罗拉匹坦; SCH619734) 目录号 : GC15449
A potent NK1 receptor antagonist
Cas No.:552292-08-7
Sample solution is provided at 25 µL, 10mM.
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Description:
Kb: 0.17 nM
Neurokinin NK1 receptors have been shown to play a role in a variety of behavioral responses in both animals and humans that has lead to the development of selective antagonists for this receptor. Principal of NK1 antagonists is their inhibitory effects against emesis induced by a variety of emetogenic stimuli. Rolapitant (SCH 619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist.
In vitro: In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over mouse, rat and rabbit. Rolapitant is a functionally competitive antagonist with a calculated Kb of 0.17 nM. [1].
In vivo: Rolapitant reversed NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose of 0.1 mg/kg. Rolapitant was efficacious at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, which is consistent with clinical data for other NK1 antagonists [1].
Clinical trial: Rolapitant is superior to placebo in reducing emetic episodes after surgery and reduces the incidence of vomiting in a dose-dependent manner. No differences were observed in side effect profile between rolapitant and placebo [2].
Reference:
[1] Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.
[2] Gan TJ, Gu J, Singla N, Chung F, Pearman MH, Bergese SD, Habib AS, Candiotti KA, Mo Y, Huyck S, Creed MR, Cantillon M; Rolapitant Investigation Group. Rolapitant for the prevention of postoperative nausea and vomiting: a prospective, double-blinded, placebo-controlled randomized trial. Anesth Analg. 2011 Apr;112(4):804-12.
Kinase experiment: | 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]. |
References: [1]. Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. | |
| Cas No. | 552292-08-7 | SDF | |
| 别名 | 罗拉匹坦; SCH619734 | ||
| 化学名 | (5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]dec-1-en-2-ol | ||
| Canonical SMILES | C[C@](OC[C@@]1(C2=CC=CC=C2)CC[C@@]3(CN1)CCC(O)=N3)([H])C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4 | ||
| 分子式 | C25H26F6N2O2 | 分子量 | 500.48 |
| 溶解度 | DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 16 mg/ml,Ethanol: 3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9981 mL | 9.9904 mL | 19.9808 mL |
| 5 mM | 0.3996 mL | 1.9981 mL | 3.9962 mL |
| 10 mM | 0.1998 mL | 0.999 mL | 1.9981 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet