A 784168
目录号 : GC17091
A TRPV1 antagonist
Cas No.:824982-41-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A 784168 is a potent antagonist of TRPV1 receptor with pKi value of 7.15 [1].
The transient receptor potential cation channel subfamily V member 1 (TrpV1) receptor is a nonselective cation channel and distributes throughout the nervous system. TrpV1 receptor is activated by a wide variety of physical and chemical stimuli [1].
A 784168 is a potent TRPV1 receptor antagonist with pKi value of 7.15 for recombinant hTRPV1 receptor. In the Ca2+ flux assay, A 784168 inhibited 50 nM CAP-induced calcium flux with pIC50 value of 7.13 of the recombinant hTRPV1 receptor [1]. A 784168 inhibited TRPV1 activation by 50 nM capsaicin, pH 5.5, 3 μM NADA and 10 μM anandamide with IC50 values of 25, 14, 33.7, 35.1 nM, respectively. In rat dorsal root ganglion neurons, A 784168 inhibited 1 μM capsaicin-induced currents with IC50 value of 10 nM [2].
In CFA-induced thermal hyperalgesia, A-784168 (30 μM/kg) reduced capsaicin-induced nocifensive behaviors with ED50 value of 10 μM/kg [2]. In rats, A 784168 inhibited 1% formalin-induced secondary mechanical hyperalgesia and allodynia in the contralateral and ipsilateral paws [3].
References:
[1]. Bianchi BR, El Kouhen R, Neelands TR, et al. [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J Pharmacol Exp Ther, 2007, 323(1): 285-293.
[2]. Cui M, Honore P, Zhong C, et al. TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J Neurosci, 2006, 26(37): 9385-9393.
[3]. Martínez-Rojas VA, Barragán-Iglesias P, Rocha-González HI, et al. Role of TRPV1 and ASIC3 in formalin-induced secondary allodynia and hyperalgesia. Pharmacol Rep, 2014, 66(6): 964-971.
| Cas No. | 824982-41-4 | SDF | |
| 化学名 | 3'-(trifluoromethyl)-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-carboxamide | ||
| Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCC(C(NC(C=C3)=CC=C3S(=O)(C(F)(F)F)=O)=O)=CC2)F | ||
| 分子式 | C19H15F6N3O3S | 分子量 | 479.4 |
| 溶解度 | <47.94mg/ml in DMSO; <23.97mg/ml in ethanol | 储存条件 | Store at RT |
| 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。 |
||
| 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 | 2.0859 mL | 10.4297 mL | 20.8594 mL |
| 5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL |
| 10 mM | 0.2086 mL | 1.043 mL | 2.0859 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。