HC-030031

製品コードS2918 バッチS291802

印刷

化学情報

Chemical Structure Synonyms TOSLAB 829227 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H21N5O3
分子量 355.39 CAS No. 349085-38-7
Solubility (25°C)* 体外 DMSO 32 mg/mL (90.04 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.
in vitro HC-030031 is a substituted theophylline derivative. This compound is a potent and selective TRPA1 inhibitor. It 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. [1]
in vivo HC-030031 can be delivered to animals orally, by inhalation, or by injection. Oral administration (100 mg/kg) of this compound 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. [2] [3]

プロトコル(参考用のみ)

キナーゼアッセイ Ca2+ Measurements of Recombinant Cell Lines
Cells are plated in 384-well plates. Cells are loaded with 1 μM Fluo-4 and 0.05% pluronic acid for 1 h at room temperature. Formalin-selectivity experiments are run with 0.003% formalin. Agonist EC50 curves used 0–25 μM AITC or 0–0.017% formalin. IC50 curves for TRPA1 antagonists are 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 are collected by using a Hamamatsu FDSS 6000 fluorescence-based plate reader and analyzed using IGOR Pro.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 100, 300 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17686976/
  • https://pubmed.ncbi.nlm.nih.gov/18954467/
  • https://pubmed.ncbi.nlm.nih.gov/22927999/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Rubiadin Mediates the Upregulation of Hepatic Hepcidin and Alleviates Iron Overload via BMP6/SMAD1/5/9-Signaling Pathway [ Int J Mol Sci, 2025, 26(3)1385] PubMed: 39941155
Curcumin suppresses cell proliferation and reduces cholesterol absorption in Caco-2 cells by activating the TRPA1 channel [ Lipids Health Dis, 2023, 22(1):6] PubMed: 36641489
Toll-like receptor 4 signaling pathway in sensory neurons mediates remifentanil-induced postoperative hyperalgesia via transient receptor potential ankyrin 1 [ Mol Pain, 2023, 19:17448069231158290] PubMed: 36733260
Potential Common Mechanisms of Cytotoxicity Induced by Amide Herbicides via TRPA1 Channel Activation [ Int J Environ Res Public Health, 2022, 19(13)7985] PubMed: 35805655
Berberine Alleviates Gastroesophageal Reflux-Induced Airway Hyperresponsiveness in a Transient Receptor Potential A1-Dependent Manner [ Evid Based Complement Alternat Med, 2022, 2022:7464147] PubMed: 35586690
Proline hydroxylase domain-containing enzymes regulate calcium levels in cardiomyocytes by TRPA1 ion channel [ Exp Cell Res, 2021, S0014-4827(21)00330-X] PubMed: 34389294
The neuro-immune interaction in airway inflammation through TRPA1 expression in CD4+ T cells of asthmatic mice [ Int Immunopharmacol, 2020, 86:106696] PubMed: 32570040
Calcium Channel α2δ1 Subunit Mediates Secondary Orofacial Hyperalgesia Through PKC-TRPA1/Gap Junction Signaling. [ J Pain, 2019, S1526-5900(19)30794-1] PubMed: 31494272
Transient Receptor Potential Ion Channels Mediate Adherens Junctions Dysfunction in a Toluene Diisocyanate-Induced Murine Asthma Model [ Toxicol Sci, 2019, 168(1):160-170] PubMed: 30517707
Transient Receptor Potential Ion Channels Mediate Adherens Junctions Dysfunction in a Toluene Diisocyanate-Induced Murine Asthma Model [ Toxicol Sci, 2019, 168(1):160-170] PubMed: 30517707

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。