HC-030031

Catalog No.S2918 Synonyms: TOSLAB 829227

For research use only.

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

CAS No. 349085-38-7

Selleck's HC-030031 has been cited by 4 Publications

Purity & Quality Control

Choose Selective TRP Channel Inhibitors

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IMR90 cells M3nqRmZ2dmO2aX;uJIF{e2G7 M2[xTVQxKG2rboO= M3jYTmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hXFKSQUGg[ZhxemW|c3XkJIlvKGi3bXHuJGlOWjlyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[WO{b3zlbY4ucW6mdXPl[EBk[WylaYXtJIlv\my3eDDh[pRmeiB2MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBidmGueYPpd{whUUN3ME2xMlgh|ryP NWO3V4gzOjJ|MkWxOVU>
HEK293 cells NHvHfJlHfW6ldHnvckBie3OjeR?= NEC0ZXJCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKFSUUFGxJINp[W6wZXyg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPpco5idWGuZHXofYRmNWmwZIXj[YQhcW62cnHj[YxtfWyjcjDjZYxkcXWvIHnu[ox2gCCkeTDGUGlRWixiSVO1NF01NjlizszN NH\VR3QzODN3NkOwOS=>
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]

Protocol (from reference)

Animal Research:[2]
  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 100, 300 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 32 mg/mL
(90.04 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 355.39
Formula

C18H21N5O3

CAS No. 349085-38-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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