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ASP 7663

  Cat. No.:  DC10558   Featured
Chemical Structure
1190217-35-6
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More than 5000 active chemicals with high quality for research!
Field of application
ASP 7663 is a selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1190217-35-6
Chemical Name: CID 44232532
Synonyms: ASP 7663;(2E)-2-[7-Fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid;(E)-[7-Fluoro-1-(2-methylpropyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]acetic acid;ASP7663;GTPL10274;BDBM50318498;ASP7663, >=98% (HPLC);2-(7-fluoro-1-isobutyl-2-oxoindolin-3-ylidene)acetic acid;(2E)-2-[7-fluoro-1-(2-methylpropyl)-2-oxoindol-3-ylidene]acetic acid;CID 44232532
SMILES: FC1=C([H])C([H])=C([H])C2/C(=C(/[H])\C(=O)O[H])/C(N(C=21)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O
Formula: C14H14FNO3
M.Wt: 263.2643
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions[1][2].
In Vivo: ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice[1]. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide[1]. ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat[1]. Animal Model: CRD model (colorectal distension in rat)[1]. Dosage: 1 and 3 mg/kg. Administration: Orally. Result: Significantly reduced the number of abdominal contractions evoked during CRD at pressures of 30, 45, and 60 mmHg. ASP7663 also reduced the number of abdominal contractions by intravenous treatment.
In Vitro: ASP7663 concentration dependently increases intracellular Ca2+ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L[1]. ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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DC70461 GSK3527497 GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.
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DC9735 SB-366791 SB-366791 is a selective and competitive VR1 (TRPV1) antagonist that is commonly used in pain research.
DC8306 RQ-00203078 RQ-00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively).
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