CP-945598 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.
CP 945598 hydrochloride(CP-945598 HCl)是一种选择性和高亲和力的CB1受体拮抗剂,结合和功能实验的Ki值分别为0.7 nM 和0.12 nM[1]。
CB1受体是G蛋白偶联的大麻素受体,主要分布在中枢和外周神经系统中,在能量稳态中起重要作用。
CP 945598剂量依赖性的逆转大麻素受体激动剂(CP 55940)引发的四个特征性中枢效应,即体温降低、抗伤害感受、运动降低和强直症。
在小鼠模型中,皮下注射17.8 mg/kg的CP 945598提高了自发活动。在Sprague- Dawley大鼠中,CP 945598以剂量和浓度依赖的方式减少食物的摄入量。10 mg/kg和30 mg/kg剂量的CP 945598分别将能量消耗增加16%和19%。此外,离体脑受体占有率以剂量相关的方式增加至33-36%。与赋形组小鼠相比,在饮食诱导的肥胖小鼠中,CP 945598减少9%的体重[2]。
参考文献:
[1]. Griffith DA, Hadcock JR, Black SC, et al. Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. J Med Chem, 2009, 52(2): 234-237.
[2]. Hadcock JR1, Griffith DA, Iredale PA, et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochem Biophys Res Commun, 2010, 394(2): 366-371.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 546.88 |
Cas No. | 686347-12-6 |
Formula | C25H25Cl2N7O·HCl |
Solubility | ≥27.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
Chemical Name | 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)purin-6-yl]-4-(ethylamino)piperidine-4-carboxamide;hydrochloride |
SDF | Download SDF |
Canonical SMILES | CCNC1(CCN(CC1)C2=NC=NC3=C2N=C(N3C4=CC=C(C=C4)Cl)C5=CC=CC=C5Cl)C(=O)N.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。 |
Description | CP-945598 HCl是CB1的选择性和高亲和力拮抗剂,Ki值为0.7 nM。 | |||||
靶点 | CB1 | CB2 | ||||
IC50 | 0.7 nM (Ki) | 7.6 μM (Ki) |
质量控制和MSDS
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