ASP7663
Based on 2 publication(s) in Google Scholar
ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.26%
- CAS 番号: 1190217-35-6
- 分子式: C14H14FNO3
- 分子量:263.26
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 ASP7663
More
生物活性
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.83 μM
Compound: 67
|
Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in membrane currents
Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in membrane currents
|
[PMID: 20356305] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
化学情報
-
CAS 番号 1190217-35-6
-
性状 Solid
-
分子量 263.26
-
分子式 C14H14FNO3
-
Color Light yellow to orange
-
SMILES
O=C(O)/C=C1C(N(CC(C)C)C2=C/1C=CC=C2F)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
J Adv Res
Transforming destructive mechanical cues into therapeutic power: Activation of PIEZO1 and TRPV4 counteracts mechano-induced damage of cellular junctions in Hailey-Hailey disease. [Abstract]2025 Nov 26:S2090-1232(25)00951-8. PMID: 41314280 -
Clin Transl Med
Dissecting the effect of ileal faecal diversion on the intestine using single-cell sequencing. [Abstract]2023 Jul;13(7):e1321. PMID: 37400975
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (189.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (279 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7985 mL | 18.9926 mL | 37.9853 mL | 94.9632 mL |
| 5 mM | 0.7597 mL | 3.7985 mL | 7.5971 mL | 18.9926 mL | |
| 10 mM | 0.3799 mL | 1.8993 mL | 3.7985 mL | 9.4963 mL | |
| 15 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL | 6.3309 mL | |
| 20 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL | 4.7482 mL | |
| 25 mM | 0.1519 mL | 0.7597 mL | 1.5194 mL | 3.7985 mL | |
| 30 mM | 0.1266 mL | 0.6331 mL | 1.2662 mL | 3.1654 mL | |
| 40 mM | 0.0950 mL | 0.4748 mL | 0.9496 mL | 2.3741 mL | |
| 50 mM | 0.0760 mL | 0.3799 mL | 0.7597 mL | 1.8993 mL | |
| 60 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL | |
| 80 mM | 0.0475 mL | 0.2374 mL | 0.4748 mL | 1.1870 mL | |
| 100 mM | 0.0380 mL | 0.1899 mL | 0.3799 mL | 0.9496 mL |
ASP7663 関連分類
HY-101907 関連分類
Powered by Bioz