HC-030031(TOSLAB-829227) - 半岛电竞官方网址

Molecular Weight (MW)	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; TOSLAB-829227; TOSLAB829227; HC-030031; HC 030031; HC030031

Molecular Weight (MW)

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; TOSLAB-829227; TOSLAB829227; HC-030031; HC 030031; HC030031

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

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

CAS NO:	349085-38-7
规格:	≥98%

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