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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
ASP7663 is an selective and orally bioavailable TRPA1 activator, acting by stimulating 5-HT release from QGP-1 cells and exhibiting an abdominal analgesic effect in vivo.
| ln Vitro |
The intracellular Ca2+ concentration of human, rat, and mouse TRPA1 expressed in HEK293 cells was concentration-dependently enhanced by ASP7663, with 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]. With an EC50 value of 72.5 (52.6–99.9) μmol/L, ASP7663 concentration-dependently increases the release of 5-HT from QGP-1 cells (EC cell lineage expressing TRPA1) [1].
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| ln Vivo |
The colon transit delay caused by loperamide in mice is greatly alleviated by ASP7663 [1]. Oral ASP7663 at 0.3 and 1 mg/kg dramatically lowers the delayed microbead ejection caused by loperamide [1]. Orally administered at 1 and 3 mg/kg, ASP7663 prevents colorectal distension in rats [1].
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| Animal Protocol |
Animal/Disease Models: CRD model (rat colorectal dilatation) [1].
Doses: 1 and 3 mg/kg. Mode of Route of Administration: Orally. Experimental Results: Significant reduction in the number of abdominal contractions induced by CRD at 30, 45 and 60 mmHg pressures. ASP7663 also diminished the number of abdominal contractions with intravenous (iv) (iv)treatment. |
| References |
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| Molecular Formula |
C14H14FNO3
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|---|---|
| Molecular Weight |
263.26
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| Exact Mass |
263.095
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| CAS # |
1190217-35-6
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| Related CAS # |
1190217-35-6
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| PubChem CID |
44232532
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| Appearance |
Light yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
368.1±42.0 °C at 760 mmHg
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| Flash Point |
176.4±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.628
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| LogP |
2.82
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CN1C2=C(C=CC=C2F)/C(=C\C(=O)O)/C1=O
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| InChi Key |
RCVZUIGCNAAMIC-UXBLZVDNSA-N
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| InChi Code |
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+
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| Chemical Name |
(2E)-2-[7-Fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid
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| Synonyms |
ASP-7663 ASP 7663ASP7663
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~189.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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