product name HC-030031
Description: HC-030031 (also known as 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. As an inhibitor of TRPA1, HC-030031 can be used as a tool to study the role of this channel in pain perception. In the FLIPR calcium-influx assay, HC-030031 blocks cinnamaldehyde- and AITC- induced activation of TRPA1 with IC50 values of 4.9μM and 7.5μM, respectively. HC-030031 is selective against TRPA1. It shows no significant inhibitory activity against many other enzymes, receptors and transporters. It also has no effect on the activation of TRPV1, TRPV3 and TRPV4.
References: Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30; Mol Pain. 2008 Oct 27;4:48. doi: 10.1186/1744-8069-4-48; PLoS One. 2012;7(8):e43597.
355.39
Formula
C18H21N5O3
CAS No.
349085-38-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 32 mg/mL (90.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% methylcellulose: 30 mg/mL
Synonyms
TOSLAB 829227
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cells were plated in 384-well plates. Cells were loaded with 1 μM Fluo-4 and 0.05% pluronic acid for 1 h at room temperature. Formalin-selectivity experiments were run with 0.003% formalin. Agonist EC50 curves used 0–25 μM AITC or 0–0.017% formalin. IC50 curves for TRPA1 antagonists were 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 were collected by using a Hamamatsu FDSS 6000 fluorescence-based plate reader and analyzed using IGOR Pro. Cell Assay: HC-030031 selectively inhibited TRPA1 activation by cinnamaldehyde and allyl isothiocyanate (AITC) in vitro [2]. HC-030031 inhibited the AITC- and formalin-induced Ca2+ increase in TRPA1-expressing cells. |
|---|---|
| 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. |
| Animal model | Male Sprague-Dawley rats |
| Formulation & Dosage | Formulated in 0.5% Methylcellulose; 100, 300 mg/kg; p.o. |
| References | Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30; Mol Pain. 2008 Oct 27;4:48. doi: 10.1186/1744-8069-4-48; PLoS One. 2012;7(8):e43597 |
