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HC-030031

Catalog No. T6530   CAS 349085-38-7
Synonyms: HC030031, TOSLAB 829227

HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

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HC-030031 Chemical Structure
HC-030031, CAS 349085-38-7
Pack Size Availability Price/USD Quantity
10 mg In stock $ 46.00
50 mg In stock $ 97.00
100 mg In stock $ 148.00
200 mg In stock $ 195.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.9%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
Targets&IC50 AITC--evoked calcium influx:6.2±0.2 μM, formalin-evoked calciμM influx:5.3±0.2 μM
Kinase Assay The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate (InvivoGen) after TLR agonist treatment is carried out.
Cell Research HC-030031 is prepared in DMSO and stored, and then diluted with appropriate medium (DMSO 0.4%) before use[2]. HEK-293 cells stably expressing human TRPA1 are plated into 384-well plates at a density of 20,000 cells/well 24 hours prior to assaying. On the day of assay, cells are loaded with 4 μM Fluo-4 dye and 0.08% pluronic acid for 1 hour at room temperature in assay buffer consisting of Hank's balanced salt solution supplemented with 20 mM HEPES, 2.5 mM probenecid, and 4% TR-40. Calcium influx assays are performed using the Fluorometric Imaging Plate Reader (FLIPR) TETRA. Concentration-response curves are generated for the TRPA1 agonists cinnamaldehyde and AITC prior to antagonist testing so EC60 concentrations could be determined. Titrations of HC-030031 are made from a DMSO stock solution and DMSO is kept to a constant of 0.4% in the assay. The antagonist is incubated with the cells for 10 minutes before the addition of an EC60 concentration of either cinnamaldehyde (18 μM) or AITC (6 μM) and calcium influx is monitored for an additional 10 minutes[2].
Animal Research Animal Models: Male Sprague-Dawley rats. Formulation: 0.5% Methylcellulose. Dosages: 100,300 mg/kg. Administration: oral administration
Synonyms HC030031, TOSLAB 829227
Molecular Weight 355.39
Formula C18H21N5O3
CAS No. 349085-38-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35.5 mg/mL (100 mM)

TargetMolReferences and Literature

1. McNamara CR, et al. Proc Natl Acad Sci, 2007, 104(33), 13525-13530. 2. Eid SR, et al. Mol Pain, 2008, 4:48. 3. Lennertz RC, et al. PLoS One. 2012;7(8):e43597. 4. Tian C, Huang R, Tang F, et al. Transient Receptor Potential Ankyrin 1 Contributes to Lysophosphatidylcholine-Induced Intracellular Calcium Regulation and THP-1-Derived Macrophage Activation[J]. The Journal of Membrane Biology. 2019: 1-13.

TargetMolCitations

1. Tian C, Huang R, Tang F, et al. Transient Receptor Potential Ankyrin 1 Contributes to Lysophosphatidylcholine-Induced Intracellular Calcium Regulation and THP-1-Derived Macrophage Activation. The Journal of Membrane Biology. 2019: 1-13

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Ion Channel Inhibitor Library NO PAINS Compound Library Anti-Cancer Compound Library Neuronal Signaling Compound Library ReFRAME Related Library Immunology/Inflammation Compound Library Target-Focused Phenotypic Screening Library

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Keywords

HC-030031 349085-38-7 Membrane transporter/Ion channel TRP/TRPV Channel TRP Channel HC030031 Transient receptor potential channels TOSLAB 829227 Inhibitor HC 030031 TOSLAB829227 inhibit TOSLAB-829227 inhibitor

 

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