S84972 |
Chembridge-5861528 |
| 源叶(MedMol) | ≥98%(HPLC) |
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- 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)
- 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： -20℃
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
