HC-030031
(Synonyms: 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺) 目录号 : GC15947
Selective TRPA1 channel blocker
Cas No.:349085-38-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
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Ca2+ Measurements of Recombinant Cell Lines |
Cells were plated in 384-well plates. Cells were loaded with 1 μM Fluo-4 and 0.05% pluronic acid for 1 h at room temperature. Formalin-selectivity experiments were run with 0.003% formalin. Agonist EC50 curves used 0–25 μM AITC or 0–0.017% formalin. IC50 curves for TRPA1 antagonists were constructed by using 0.625–40 μM antagonist in the presence of 5 μM AITC or 0.001% formalin using data collected 3 min after agonist addition. Data were collected by using a Hamamatsu FDSS 6000 fluorescence-based plate reader and analyzed using IGOR Pro. |
| Cell experiment: | |
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Cell lines |
TRPA1-expressing HEK293 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10 μM for 3 min |
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Applications |
HC-030031 selectively inhibited TRPA1 activation by cinnamaldehyde and allyl isothiocyanate (AITC) in vitro [2]. HC-030031 inhibited the AITC- and formalin-induced Ca2+ increase in TRPA1-expressing cells [1]. |
| Animal experiment: | |
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Animal models |
Male Sprague-Dawley rats model |
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Dosage form |
100 or 300 mg/kg; p.o. for 60 min; |
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Applications |
HC-030031 reduced inflammatory- and neuropathy-induced mechanical hypersensitivity. HC-030031 attenuated formalin- and allyl isothiocyanate-evoked pain behavior via inhibition of TRPA1 [2]. Moreover, HC-030031 alleviated behavioral mechanical hyperalgesia without affecting heat hyperalgesia in inflamed mice [3]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1McNamara, C. R., Mandel-Brehm, J., Bautista, D. M., Siemens, J., Deranian, K. L., Zhao, M., Hayward, N. J., Chong, J. A., Julius, D., Moran, M. M. and Fanger, C. M. (2007) TRPA1 mediates formalin-induced pain. Proc Natl Acad Sci U S A. 104, 13525-13530 2Eid, S. R., Crown, E. D., Moore, E. L., Liang, H. A., Choong, K. C., Dima, S., Henze, D. A., Kane, S. A. and Urban, M. O. (2008) HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol Pain. 4, 48 3Lennertz, R. C., Kossyreva, E. A., Smith, A. K. and Stucky, C. L. (2012) TRPA1 mediates mechanical sensitization in nociceptors during inflammation. PLoS One. 7, e43597 |
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HC-030031 is a selective antagonist of transient receptor potential ankyrin subfamily, member 1(TRPA1) with IC50 value of 4.9μM [1].
TRP channels are found to take participate in the response of chemical stimuli and in mechanoreception. TRPA1 is the sole mammalian member of TRPA subfamily. As an inhibitor of TRPA1, HC-030031 can be used as a tool to study the role of this channel in pain perception. In the FLIPR calcium-influx assay, HC-030031 blocks cinnamaldehyde- and AITC- induced activation of TRPA1 with IC50 values of 4.9μM and 7.5μM, respectively. HC-030031 is selective against TRPA1. It shows no significant inhibitory activity against many other enzymes, receptors and transporters. It also has no effect on the activation of TRPV1, TRPV3 and TRPV4. In vivo, HC-030031 significantly reduces the hindpaw lifting induced by AITC as well as mechanical hypersensitivity induced by CFA in rats. Besides that, the administration of HC-030031(300mg/kg) can markedly attenuate the hypersensitivity (41%) induced by spinal nerve ligation [1].
References:
[1] Eid S R, Crown E D, Moore E L, et al. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory-and neuropathy-induced mechanical hypersensitivity. Mol Pain, 2008, 4(48): 1-10.
| Cas No. | 349085-38-7 | SDF | |
| 别名 | 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺 | ||
| 化学名 | 2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(4-propan-2-ylphenyl)acetamide | ||
| Canonical SMILES | CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C | ||
| 分子式 | C18H21N5O3 | 分子量 | 355.39 |
| 溶解度 | ≥ 16.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8138 mL | 14.0691 mL | 28.1381 mL |
| 5 mM | 0.5628 mL | 2.8138 mL | 5.6276 mL |
| 10 mM | 0.2814 mL | 1.4069 mL | 2.8138 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。