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Submit ReviewA 425619
说明： Potent TRPV1 antagonist
化学名： N-5-Isoquinolinyl-N'-[[(4-(trifluoromethyl)phenyl]methyl]urea
纯度： ≥98% (HPLC)
生物活性 for A 425619
A 425619 is a potent TRPV1 antagonist (IC50 = 3-9 nM). Blocks capsaicin-evoked currents in rat DRG neurons and inhibits TRPV1-activation by anandamide (Cat. No. 1339) and N-arachidonoyl-dopamine. Reduces pain in inflammatory, postoperative and osteoarthritic in vivo pain models.
化合物库 for A 425619
A 425619 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for A 425619
| 分子量 | 345.32 |
| 公式 | C18H14F3N3O |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 581809-67-8 |
| PubChem ID | 8068410 |
| InChI Key | SJGVXVZUSQLLJB-UHFFFAOYSA-N |
| Smiles | O=C(NCC1=CC=C(C(F)(F)F)C=C1)NC2=CC=CC3=CN=CC=C32 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for A 425619
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 34.53 | 100 | |
| ethanol | 34.53 | 100 |
制备储备液 for A 425619
以下数据基于产品分子量 345.32。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.9 mL | 14.48 mL | 28.96 mL |
| 5 mM | 0.58 mL | 2.9 mL | 5.79 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.9 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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产品说明书 for A 425619
参考文献 for A 425619
参考文献是支持产品生物活性的出版物。
El Kouhen et al (2005) A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid. J.Pharmacol.Exp.Ther. 314 400 PMID: 15837819
McGaraughty et al (2006) Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats. J.Neurophysiol. 95 18 PMID: 16162831
If you know of a relevant reference for A 425619, please let us know.
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关键词: A 425619, A 425619 supplier, A425619, TRPV1, antagonists, antagonism, transient, receptor, potential, channels, vanilloids, pain, nociception, capsaicin, TRPV, 5781, Tocris Bioscience
2 篇 A 425619 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 425619 的部分引用包括：
Jong-Woo et al (2022) Melanocortin-4 receptors activate sympathetic preganglionic neurons and elevate blood pressure via TRPV1. Cell Rep 41 111579 PMID: 36323255
Chakrabarti et al (2018) Acute inflammation sensitizes knee-innervating sensory neurons and decreases mouse digging behavior in a TRPV1-dependent manner. Neuropharmacology 143 49 PMID: 30240782
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A 425619 的评论
平均评分: 4 (Based on 1 Review.)
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Inhibiting calcium entry in human mast cells stimulated with cortistatin.
By
ANANTH KUMAR KAMMALA on 01/30/2021
分析类型： In Vitro
种属： Human
细胞系/组织： LAD2 - mast cells
A425619 product was used to study the role of MrgprX2 receptor in calcium mobilization in human mast cells. At a concentration of 0.01 and 0.03uM A425619 inhibited calcium entry significantly when stimulated mast cells with cortistatin.
