MCE 的所有產(chǎn)品僅用作科學研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

HC-030031

CAS No. : 349085-38-7

產(chǎn)品活性：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.

研究領(lǐng)域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶點：TRP Channel

In Vitro: HC-030031 reversibly blocks TRPA1 currents with a similar potency, regardless of the agonist used; this includes blockade of currents elicited by reversible agonists, such as AITC, or irreversible agonists, such as N-methyl maleimide. HC-030031 blocks activation of TRPA1 by N-methyl maleimide, which opens the channel irreversibly through cysteine modification. HC-030031 does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG, or NaV1.2 channels. The potencies of HC-030031 versus cinnamaldehyde or allyl isothiocyanate (AITC or Mustard oil)-induced TRPA1 activation are 4.9±0.1 and 7.5±0.2 μM respectively (IC₅₀). These findings are similar to the previously reported IC₅₀ of 6.2 μM against AITC activation of TRPA1. The ability of HC-030031 to block TRPA1 activation is tested in a FLIPR calcium-influx assay using HEK-293 cells stably expressing human TRPA1. Concentrations of HC-030031 from 0.3 to 60 μM are incubated with cells for 10 minutes prior to addition of an EC₆₀ concentration of either cinnamaldehyde or AITC. HC-030031 dose-dependently blocks cinnamaldehyde- and AITC-induced calcium influx with IC₅₀ values of 4.9 and 7.5 μM, respectively.

In Vivo: 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).

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Membrane Transporter/Ion Channel Compound Library  |  Neuronal Signaling Compound Library  |  Mechanoreceptors Compound Library  |  Human Metabolite Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Bisandrographolide C  |  TRPV1 activator-2  |  SB-705498  |  AMTB hydrochloride  |  ABT-239  |  AS1269574  |  Tivanisiran  |  RN-1747  |  CEDAEVFKDSMVPGEK  |  Asivatrep  |  TRPV4 agonist-1  |  GsMTx4 TFA  |  SET2  |  (E)-4-Oxo-2-nonenal  |  1-Stearoyl-2-arachidonoyl-sn-glycerol  |  Podocarpic acid  |  M8-B  |  Pregnenolone monosulfate sodium  |  TRPC5 modulator-1  |  Capsiate  |  Diisopropyl adipate  |  FEMA 4809  |  Capsazepine  |  JT010  |  Umbellulone  |  ML-SI1  |  TRPC5-IN-4  |  EIPA hydrochloride  |  GSK2193874  |  Icilin

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種全球僅有化合物庫，我們致力于為全球科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實驗中心和嚴格的質(zhì)控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團隊跟蹤最新的制藥及生命科學研究進展，為您提供全球新的活性化合物；
•   與世界各大制藥公司及著名科研機構(gòu)建立了長期的合作。