| 产品描述： | Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC50 values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities |
| 靶点： |
TRPA1:14.3 μM (IC50, allyl isothiocyanate-evoked TRPA1 response);TRPA1:18.7 μM (IC50, 4-HNE-evoked TRPA1 response);TRP/TRPVChannel |
| 体外研究： |
Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM |
| 体内研究： |
Chembridge-5861528 (TCS 5861528) (30 mg/kg; i.p.; twice daily for a week) significantly attenuates development of mechanical hypersensitivity in Streptozocin (HY-13753)-induced diabetes mellitus rat model. Chembridge-5861528 (3 and 10 μg/rat; i.t.; once) attenuates Capsaicin (HY-10448)-induced blood flow increase in a dose-related fashion. Animal Model: Male Hannover-Wistar rats, Streptozocin-induced diabetes mellitus model Dosage: 30 mg/kg Administration: Intraperitoneal injection, twice daily for a week Result: Significantly attenuated development of mechanical hypersensitivity as revealed by the paw pressure test (F1,80= 31.4, P < 0.0001). Animal Model: Male Hannover–Wistar rats (220-260 g), Capsaicin-induced neurogenic inflammation model Dosage: 0, 3, and 10 μg/rat Administration: Intrathecal injection, 20 min before Capsaicin injection Result: Significantly decreased the blood flow at 10 μg. |
| 参考文献： |
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. Spinal TRPA1 ion channels contribute to cutaneous neurogenic inflammation in the rat. Neurosci Lett. 2010 Aug 2;479(3):253-6. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.707 ml |
13.535 ml |
27.07 ml |
| 5 mM |
0.541 ml |
2.707 ml |
5.414 ml |
| 10 mM |
0.271 ml |
1.353 ml |
2.707 ml |
| 50 mM |
0.054 ml |
0.271 ml |
0.541 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京