research use only
Cat.No.S2918
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor ATPase GluR |
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| Other TRP Channel Inhibitors | SKF96365 AMG-517 2-APB (2-Aminoethyl Diphenylborinate) GSK2193874 Capsazepine GSK1016790A SB705498 Caffeic Acid EIPA (L593754) HC-067047 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| IMR90 cells | Function assay | 40 mins | Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis, IC50=1.8 μM | |||
| HEK293 cells | Function assay | Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx by FLIPR, IC50=4.9 μM | ||||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 71 mg/mL
(199.78 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 355.39 | Formula | C18H21N5O3 |
Storage (From the date of receipt) | |
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| CAS No. | 349085-38-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | TOSLAB 829227 | Smiles | CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C | ||
| Targets/IC50/Ki |
TRPA1
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| 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.
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| 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.
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References |
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