1190217-35-6

1190217-35-6 structure

Name: ASP 7663
Chemical Name: (2E)-(7-Fluoro-1-isobutyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)acetic acid
CAS Number: 1190217-35-6
Molecular Formula: C₁₄H₁₄FNO₃
Molecular Weight: 263.264
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2018-05-20 08:00:00
Modify Date: 2024-01-06 10:44:59
ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions[1][2].

Name	(2E)-(7-Fluoro-1-isobutyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)acetic acid
Synonyms	(2E)-(7-Fluoro-1-isobutyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)acetic acid Acetic acid, 2-[7-fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]-, (2E)- ASP 7663

Description	ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions[1][2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Neurological Disease
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].
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.
References	[1]. Ryosuke Kojima, et al. Effects of Novel TRPA1 Receptor Agonist ASP7663 in Models of Drug-Induced Constipation and Visceral Pain. Eur J Pharmacol. 2014 Jan 15;723:288-93. [2]. Yao Lu, et al. Transient Receptor Potential Ankyrin 1 Activation Within the Cardiac Myocyte Limits Ischemia-reperfusion Injury in Rodents. Anesthesiology. 2016 Dec;125(6):1171-1180.

Density	1.4±0.1 g/cm3
Boiling Point	368.1±42.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₄FNO₃
Molecular Weight	263.264
Flash Point	176.4±27.9 °C
Exact Mass	263.095764
LogP	2.82
Vapour Pressure	0.0±0.9 mmHg at 25°C
Index of Refraction	1.628

RIDADR	NONH for all modes of transport

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.

1190217-35-6	134282-93-2
906737-25-5	141663-36-7
5513-86-0	828288-98-8
47091-50-9	112230-24-7
188849-34-5	137506-04-8
1522743-03-8	1518063-06-3
1533619-82-7	1502312-97-1
1622180-53-3	1519539-52-6
1260897-06-0	1260872-90-9
1622180-57-7	1622180-55-5