ASP 7663|cas 1190217-35-6|DC Chemicals

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].

Cat. No.	Product name	Field of application
DC72365	BAY-390	BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively.
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.
DC70460	GSK3395879	GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4); exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6); demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.
DC11472	TRPM8 antagonist 14	TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
DC7755	TRCP6 inhibitor(SAR7334)	TRPC6 inhibitor is a potent TRPC6(Transient receptor potential cation channel, subfamily C, member 6) inhibitor.
DC9722	SKF96365	SKF96365 is blocker of TRP cation channels. Inhibits capacitative Ca2+ entry.
DC9635	SB-705498	SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
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).
DC7262	Optovin	Optovin is a reversible photoactive TRPA1 activator.