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HC-030031(TOSLAB-829227)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HC-030031(TOSLAB-829227)图片
CAS NO:349085-38-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)355.39
FormulaC18H21N5O3
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
SynonymsTOSLAB 829227; TOSLAB-829227; TOSLAB829227; HC-030031; HC 030031; HC030031
实验参考方法
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 VivoHC-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 modelMale Sprague-Dawley rats
Formulation & DosageFormulated 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