TCS 5861528 (TCS 5861528) 是一种有效的 TRPA1 通道拮抗剂,可拮抗类似的异硫氰酸烯丙酯和 4-HNE 诱发的 TRPA1 反应,IC50 值分别为 14.3 μM 和 18.7 μM。
Cas No. | 332117-28-9 |
别名 | TCS 5861528 |
化学名 | (R)-N-(4-(sec-butyl)phenyl)-2-(1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)acetamide |
Canonical SMILES | O=C1N(C)C(N(C)C(N=C2)=C1N2CC(NC3=CC=C(C=C3)[C@H](C)CC)=O)=O |
分子式 | C19H23N5O3 |
分子量 | 369.42 |
溶解度 | ≥ 76 mg/mL in DMSO with ultrasonic and warming, ≥ 6.17 mg/mL in EtOH with ultrasonic and warming |
储存条件 | Store at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively). References: [1]. Wei H, et al. Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology. 2009 Jul;111(1):147-54. [2]. Wei H, et al. Roles of cutaneous versus spinal TRPA1 channels in mechanical hypersensitivity in the diabetic or mustard oil-treated non-diabetic rat. Neuropharmacology. 2010 Mar;58(3):578-84. [3]. Wei H, et al. Spinal TRPA1 ion channels contribute to cutaneous neurogenic inflammation in the rat. Neurosci Lett. 2010 Aug 2;479(3):253-6. |