HC-030031

Synonyms: TOSLAB 829227

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.

HC-030031 Chemical Structure

HC-030031 Chemical Structure

CAS: 349085-38-7

Selleck's HC-030031 has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

HC-030031 Related Products

Choose Selective TRP Channel Inhibitors

Cell Data

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 22325155
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 20356305
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Targets
TRPA1 [1]
In vitro
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
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]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 100, 300 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 355.39 Formula

C18H21N5O3

CAS No. 349085-38-7 SDF Download HC-030031 SDF
Smiles CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (199.78 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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