HC-030031 (TOSLAB-829227)

Alias: TOSLAB 829227;TOSLAB-829227; TOSLAB829227; HC-030031; HC 030031; HC030031
Cat No.:V0023 Purity: ≥98%
HC-030031 (also known as TOSLAB 829227)is a novel, potent and selective blocker/antagonist/inhibitor of TRPA1 (transient receptor potential ankyrin 1) channel.
HC-030031 (TOSLAB-829227) Chemical Structure CAS No.: 349085-38-7
Product category: TRP Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

HC-030031 (also known as TOSLAB 829227) is a novel, potent and selective blocker/antagonist/inhibitor of TRPA1 (transient receptor potential ankyrin 1) channel. It antagonizes AITC (allyl isothiocyanate)- 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 TRPA1 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Irreversible agonists (like N-methylmaleimide) or reversible agonists (like AITC) can both cause blockade of TRPA1 currents, and HC-030031 reversibly blocks them with potencies of equal magnitude. N-methylmaleimide activates TRPA1, and HC-030031 prevents this from happening. This modification of the cysteine opens the channel irreversibly. TRPV1, TRPV3, TRPV4, hERG, and NaV1.2 channel-mediated currents are not blocked by HC-030031 [1]. For TRPA1 activation induced by cinnamaldehyde or allyl isothiocyanate (AITC or mustard oil), the potency of HC-030031 was 4.9 and 7.5 μM (IC50), respectively. The IC50 of 6.2 μM for the AITC activation of TRPA1 reported earlier is comparable to these results. In the FLIPR calcium influx assay, which employs HEK-293 cells that stable express human TRPA1, the capacity of HC-030031 to inhibit TRPA1 activation was examined. Before adding EC60 concentrations of either AITC or cinnamonaldehyde, HC-030031 at concentrations ranging from 0.3 to 60 μM was incubated with cells for 10 minutes. In a dose-dependent manner, HC-030031 inhibits the calcium influx induced by both cinnamonaldehyde and AITC, with IC50 values of 4.9 and 7.5 μM, respectively [2].
ln Vivo
After injecting 10% AITC (50 μL) into the hind paws of rats, HC-030031 (300 mg/kg) significantly decreased the amount of flinching within the first five minutes. For the remainder of the hour, HC-030031 decreased the frequency of withdrawals, which was similar to the effect seen in withdrawals induced by formalin [1]. At 100 mg/kg, oral HC-030031 administration decreased AITC-induced nociceptive behavior in rats. Additionally, in a more chronic model of complete Freund's adjuvant (CFA)-induced inflammatory pain as well as in a spinal nerve ligation model of neuropathic pain, oral administration of HC-030031 (100 mg/kg) significantly reversed mechanical hypersensitivity. One hour following oral administration, HC-030031 dramatically reduced the elevation's duration (p<0.001)[2]. Inflamed mice that receive HC-030031 fully recover from enhanced mechanical discharge [3].
Animal Protocol
Formulated in 0.5% Methylcellulose; 100, 300 mg/kg; p.o.
Male Sprague-Dawley rats
References
[1]. McNamara CR, et al. TRPA1 mediates formalin-induced pain. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30.
[2]. Eid SR, et al. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol Pain. 2008 Oct 27;4:48.
[3]. Lennertz RC, et al. TRPA1 mediates mechanical sensitization in nociceptors during inflammation. PLoS One. 2012;7(8):e43597.
[4]. Miyake T, et al. Cold sensitivity of TRPA1 is unveiled by the prolyl hydroxylation blockade-induced sensitization to ROS. Nat Commun. 2016 Sep 15;7:12840.
[5]. So K, et al. Hypoxia-induced sensitisation of TRPA1 in painful dysesthesia evoked by transient hindlimb ischemia/reperfusion in mice. Sci Rep. 2016 Mar 17;6:23261
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H21N5O3
Molecular Weight
355.39
CAS #
349085-38-7
SMILES
O=C1C2=C(N=C([H])N2C([H])([H])C(N([H])C2C([H])=C([H])C(=C([H])C=2[H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)N(C([H])([H])[H])C(N1C([H])([H])[H])=O
Synonyms
TOSLAB 829227;TOSLAB-829227; TOSLAB829227; HC-030031; HC 030031; HC030031
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8138 mL 14.0691 mL 28.1381 mL
5 mM 0.5628 mL 2.8138 mL 5.6276 mL
10 mM 0.2814 mL 1.4069 mL 2.8138 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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