1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. ASP7663

ASP7663 

Cat. No.: HY-101907
Handling Instructions

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.

For research use only. We do not sell to patients.

ASP7663 Chemical Structure

ASP7663 Chemical Structure

CAS No. : 1190217-35-6

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Description

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions[1][2].

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.
Molecular Weight

263.26

Formula

C₁₄H₁₄FNO₃

CAS No.

1190217-35-6

SMILES

O=C(O)/C=C1C(N(CC(C)C)C2=C/1C=CC=C2F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (949.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7985 mL 18.9926 mL 37.9853 mL
5 mM 0.7597 mL 3.7985 mL 7.5971 mL
10 mM 0.3799 mL 1.8993 mL 3.7985 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ASP7663ASP 7663ASP-7663TRP ChannelTransient receptor potential channelspainInhibitorinhibitorinhibit

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Product name:
ASP7663
Cat. No.:
HY-101907
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