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Chembridge-5861528

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Chemical Structure| 332117-28-9 同义名 : TCS 5861528
CAS号 : 332117-28-9
货号 : A209665
分子式 : C19H23N5O3
纯度 : 99%+
分子量 : 369.418
MDL号 : MFCD01993436
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 115 mg/mL(311.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 TRPA1 ion channel, expressed in nociceptive primary afferent neurons, modulates excitability of nociceptors, and it may be activated by compounds resulting from oxidative insults. DM (diabetes mellitus) increases 4-HNE production, an endogenous product of oxidative stress, which activates the TRPA1 channel[3]. Chembridge-5861528 is a reversible TRPA1 channel antagonist. Intrathecal (i.t.) administration of Chembridge-5861528 at doses 2.5-5.0 μg/rat markedly attenuated diabetic hypersensitivity, whereas 20 μg of Chembridge-5861528 was needed to produce a weak attenuation of diabetic hypersensitivity with intraplantar (i.pl.) administrations. In controls, i.pl. administration of Chembridge-5861528 (20 μg) produced a weak antihypersensitivity effect at the mustard oil-treated site. I.t. administration of Chembridge-5861528 (10 μg) in controls produced a strong antihypersensitivity effect adjacent to the mustard oil-treated area (site of secondary hyperalgesia)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Wei H, Chapman 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.

[2]Wei H, Hamalainen MM, et al. Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology. 2009 Jul;111(1):147-54.

[3]Wei H, Hämäläinen MM, Saarnilehto M, Koivisto A, Pertovaara A. Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology. 2009;111(1):147-154

[4]Wei H, Chapman H, Saarnilehto M, Kuokkanen K, Koivisto A, Pertovaara A. Roles of cutaneous versus spinal TRPA1 channels in mechanical hypersensitivity in the diabetic or mustard oil-treated non-diabetic rat. Neuropharmacology.2010;58(3):578-584