Rolapitant HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Kb:0.17 nM
在动物与人类中,神经激肽NK1受体参与一系列行为学反应,因而导致多种选择性NK1受体拮抗剂的发展.NK1拮抗剂主要抑制各种致吐刺激引起的呕吐.Rolapitant(SCH619734)是一种有效的\选择性的以及口服有效的神经激肽NK1受体拮抗剂.
体外:Rolapitant HCl对人NK1受体具有较高的亲和性(0.66 nM),比对人NK2和NK3的选择性高1000多倍.此外,相对于小鼠\大鼠以及兔子,Rolapitant HCl对人\豚鼠\沙鼠以及猴的NK1受体具有较高的亲和力.Rolapitant HCl是一种功能竞争性拮抗剂,其计算的Kb值为0.17 nM[1].
体内:静脉注射和口服给予沙鼠最小有效剂量(0.1 mg/kg)的Rolapitant HCl,持续24小时,可逆转NK1激动剂诱导的顿足.在雪貂急性以及延迟性呕吐模型中,Rolapitant HCl的有效剂量为0.1 mg/kg和1 mg/kg,与其它NK1受体拮抗剂的临床数据一致[1].
临床试验:Rolapitant HCl较安慰剂更有利于减少外科手术后的呕吐发作,并呈剂量依赖性地减少呕吐的发生率.Rolapitant HCl与安慰剂的副作用之间没有显著差异[2].
参考文献：
[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.
| Storage | Store at -20°C |
| M.Wt | 536.94 |
| Cas No. | 552292-08-7 (free base) |
| Formula | C25H27ClF6N2O2 |
| Solubility | insoluble in H2O; ≥28.7 mg/mL in EtOH with ultrasonic; ≥32.9 mg/mL in DMSO |
| Chemical Name | (5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]dec-1-en-2-ol hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C[C@]([H])(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)OC[C@]2(CC[C@]3(CCC(O)=N3)CN2)C4=CC=CC=C4.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
