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• 产品描述： HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

• 靶点： TRPA1

• 体内研究： After injection of AITC (50 μL of 10%) into the rat hind paw, HC-030031 (300 mg/kg) significantly reduces flinching during the first 5 min. Over the remainder of the hour, HC-030031 decreases flinch frequency, a result that mirrors the effects observed on formalin-induced flinching. In the rat, oral administration of HC-030031 reduces AITC-induced nocifensive behaviors at a dose of 100 mg/kg. Moreover, oral HC-030031 (100 mg/kg) significantly reverses mechanical hypersensitivity in the more chronic models of Complete Freunds Adjuvant (CFA)-induced inflammatory pain and the spinal nerve ligation model of neuropathic pain. One hour post-oral administration, HC-030031 significantly reduces the lifting duration following 1% AITC injection (p<0.001). HC-030031 completely reverses the enhanced mechanical firing in inflamed mice (p<0.001)

• 参考文献：
  1. McNamara CR, et al. TRPA1 mediates formalin-induced pain. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30. 2. Eid SR, et al. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol Pain. 2008 Oct 27;4:48. 3. Lennertz RC, et al. TRPA1 mediates mechanical sensitization in nociceptors during inflammation. PLoS One. 2012;7(8):e43597. 4. Miyake T, et al. Cold sensitivity of TRPA1 is unveiled by the prolyl hydroxylation blockade-induced sensitization to ROS. Nat Commun. 2016 Sep 15;7:12840. 5. So K, et al. Hypoxia-induced sensitisation of TRPA1 in painful dysesthesia evoked by transient hindlimb ischemia/reperfusion in mice. Sci Rep. 2016 Mar 17;6:23261.

• 溶解性： DMSO  :  25  mg/mL  (70.35  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.814 ml	14.069 ml	28.138 ml
  5 mM	0.563 ml	2.814 ml	5.628 ml
  10 mM	0.281 ml	1.407 ml	2.814 ml
  50 mM	0.056 ml	0.281 ml	0.563 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *