HC-030031CAS号： 349085-38-7分子式： C18H21N5O3分子量： 355.39描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
HC-030031是一种选择性的TRPA1通道阻断剂，可以拮抗AITC和formalin引起的钙流入，IC50分别为6.2μM和5.3μM。HC-030031能快速且可逆阻断AITC或Formalin引起的内向和外向电流，也能抑制N-methylmaleimide和Electrophillic前列腺素引起的TRPA1激活。HC-030031不抑制TRPV1, TRPV3, TRPV4 hERG, 或NaV1.2通道介导的电流。 |
| 纯度 |
≥99%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
HC030031
|
| 外观 |
白色至淡黄色粉末
|
| 可溶性/溶解性 |
DMSO : 35.5 mg/mL (100 mM))
|
| 生物活性 | |
| 靶点 |
TRPA1
|
| In vitro(体外研究) |
HC-030031 is a substituted theophylline derivative. Potent and selective TRPA1 inhibitor. HC-030031 can block both inward and outward currents elicited by AITC or formalin rapidly and reversibly and also blocks the activation of TRPA1 by N-methylmaleimide and by electrophillic prostaglandins. It does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels.
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| In vivo(体内研究) |
HC-030031 can be delivered to animals orally, by inhalation, or by injection. Oral administration (100 mg/kg) of HC-030031 significantly reversed mechanical hypersensitivity in rat models of chronic inflammatory or neuropathic pain, while local injection (100 μg) into inflamed mouse hind paws attenuated mechanical, but not heat, hypersensitivity.
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| 参考文献 | |
| 参考文献 |
TRPA1 mediates mechanical sensitization in nociceptors during inflammation.
Lennertz RC,et al. PLoS One. 2012;7(8):e43597. PMID: 22927999. H 䔸Żᩄ 族痛셌Ų 族痛셌Ų Item 褐 Count ๏ 趌๐ 侮靴 ᠠi S ñ ñ 眘⮦眀⮦敲痛๏ࠃ 馸鳘祖Item ƞƞ Count 洣盜᬴叫㺍痭ᠠ靴i 縉 靴蘿敌ଧ靴ᠠi ᭰叫㺍痭ᡸ顴먲ନ魈 鸤�ଭ鶔 懲 랖ନ؈ 煮 ﭬz�ଭ鶔 삲W鸤 ᨼĊ 煮 섈W豈勤섫W豈́煮ﭬz 섪W섲Ẃ褐ﭔz ᇈ MoveEof ƞƞ ꯍ�혐珂 劬盜蠊똉Ⴚ啑盜ᦤ叫㺍痭ᠠ靴i 侮褐 靴婢敌ଧ靴ᠠi 靴䢸Ş 䢸Ş ⌅痜Ѐ ꁠ๒⌅痜 Ѐ 䢸Ş쿹痮Љ 䕄Ż 顴蘿ॡ痮 |
分子结构图
