Description
ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
Product information
CAS Number: 1190217-35-6
Molecular Weight: 263.26
Formula: C14H14FNO3
Chemical Name: 2-[(3E)-7-fluoro-1-(2-methylpropyl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]acetic acid
Smiles: CC(C)CN1C2=C(F)C=CC=C2/C(=C\C(O)=O)/C1=O
InChiKey: RCVZUIGCNAAMIC-UXBLZVDNSA-N
InChi: InChI=1S/C14H14FNO3/c1-8(2)7-16-13-9(4-3-5-11(13)15)10(14(16)19)6-12(17)18/h3-6,8H,7H2,1-2H3,(H,17,18)/b10-6+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (949.63 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
In Vivo:
ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide. ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat.
Products are for research use only. Not for human use.
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