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Synonyms | TOSLAB 829227 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H21N5O3 |
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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 | |||
* <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. |
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. |
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in vitro | 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. [1] |
in vivo | 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. [2] [3] |
キナーゼアッセイ | Ca2+ Measurements of Recombinant Cell Lines | |
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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. |
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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。