JNJ 17203212
(Synonyms: 4-(3-(三氟甲基)吡啶-2-基)-N-(5-三氟甲基)吡啶-2-基)哌嗪-1-甲酰胺) 目录号 : GC15427
A TRPV1 antagonist
Cas No.:821768-06-3
Sample solution is provided at 25 µL, 10mM.
JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.IC50 value: 65 nM (human TRPV1), 102 nM (rat TRPV1)Target: TRPVin vivo: JNJ-17203212 reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. Throughout this study, colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle. [1] Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents core hypothermia evoked by sc capsaicin. Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents capsaicin-evoked hypothermia in a dose-response manner. [2]
References:
[1]. Wiskur BJ, et al. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats. Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64.
[2]. Swanson DM, et al. Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem. 2005 Mar 24;48(6):185
Cas No. | 821768-06-3 | SDF | |
别名 | 4-(3-(三氟甲基)吡啶-2-基)-N-(5-三氟甲基)吡啶-2-基)哌嗪-1-甲酰胺 | ||
化学名 | 4-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-carboxamide | ||
Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCN(C(NC3=NC=C(C(F)(F)F)C=C3)=O)CC2)F | ||
分子式 | C17H15F6N5O | 分子量 | 419.32 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 储存条件 | Store at -20°C |
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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。 |
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1 mg | 5 mg | 10 mg |
1 mM | 2.3848 mL | 11.9241 mL | 23.8481 mL |
5 mM | 0.477 mL | 2.3848 mL | 4.7696 mL |
10 mM | 0.2385 mL | 1.1924 mL | 2.3848 mL |
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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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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。
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