HC-030031

Catalog No.S2918

HC-030031 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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HC-030031 Chemical Structure

HC-030031 Chemical Structure
Molecular Weight: 355.39

Validation & Quality Control

Quality Control & MSDS

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HC-030031 is available in the following compound libraries:

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Product Description

Biological Activity

Description HC-030031 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]
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]
Features

Protocol(Only for Reference)

Kinase Assay: [2]

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.

Animal Study: [2]

Animal Models Male Sprague-Dawley rats
Formulation 0.5% Methylcellulose
Dosages 100, 300 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] McNamara CR, et al. Proc Natl Acad Sci, 2007, 104(33), 13525-13530.

[2] Eid SR, et al. Mol Pain, 2008, 4:48.

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Chemical Information

Download HC-030031 SDF
Molecular Weight (MW) 355.39
Formula

C18H21N5O3

CAS No. 349085-38-7
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms TOSLAB 829227
Solubility (25°C) * In vitro DMSO 32 mg/mL (90.04 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose 30 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.
Chemical Name 7H-Purine-7-acetamide, 1,2,3,6-tetrahydro-1,3-dimethyl-N-[4-(1-methylethyl)phenyl]-2,6-dioxo-

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.

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