A 784168
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.
A 784168是TRPV1受体的强效拮抗剂，pKi值为7.15[1]。
瞬时受体电位阳离子通道亚家族V1（TrpV1）受体是一种非选择性阳离子通道，分布在整个神经系统内。TrpV1受体可被各种各样的物理和化学刺激激活[1]。
A 784168是TRPV1受体的有效拮抗剂，对重组hTRPV1受体的pKi值为7.15。在Ca2+流实验中，A 784168抑制50 nM辣椒素诱导的钙内流，对重组hTRPV1受体的pIC50值为7.13[1]。A 784168抑制50 nM辣椒素、pH5.5、3 μM NADA和10 μM花生四烯酸乙醇胺诱导的TRPV1活化，IC50值分别为25、14、33.7和35.1 nM。在大鼠背根神经节神经元中，A 784168抑制1 μM辣椒素诱导的电流，IC50值为10 nM [2]。
在CFA诱导的热痛觉过敏中，30 μM/kg的A-784168减少辣椒素诱导的疼痛反应行为，ED50 为10 μM/kg [2]。在大鼠中，A 784168抑制1％福尔马林诱导的对侧和同侧爪的二次机械痛觉过敏和异常性疼痛 [3]。
参考文献：
[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.
| Physical Appearance | Off-white solid |
| Storage | Store at RT |
| M.Wt | 479.4 |
| Cas No. | 824982-41-4 |
| Formula | C19H15F6N3O3S |
| Solubility | <47.94mg/ml in DMSO; <23.97mg/ml in ethanol |
| Chemical Name | 3'-(trifluoromethyl)-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCC(C(NC(C=C3)=CC=C3S(=O)(C(F)(F)F)=O)=O)=CC2)F |
| 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。 |
化学结构
