Felcisetrag
Based on 1 publication(s) in Google Scholar
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
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- Purity: 99.94%
- CAS No.: 916075-84-8
- 화학식: C25H37N5O3
- 분자량:455.59
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Felcisetrag
MoreAll 5-HT Receptor Isoforms
More
Biological Activity
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huamn 5-HT4(c) Receptor 9.4 (pKi) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.5 nM
Compound: TD-8954
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Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
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[PMID: 26363507] |
Felcisetrag produces an elevation of cAMP in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50 = 9.3), and contracts the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50 = 8.6). Felcisetrag has moderate intrinsic activity in the vitro assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Felcisetrag (0.03~10 mg/kg; intraduodenal administration) evokes a dose-dependent relaxation of the esophagus[1].
Felcisetrag (10 and 30 μg/kg; p.o) produces an increase in contractility of the antrum, duodenum, and jejunum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs[1]
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Dosage:0.03~3 mg/kg
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Administration:S.c.
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Result:Increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
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Animal Model:Rats[1]
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Dosage:0.03~10 mg/kg
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Administration:Intraduodenal administration
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Result:Evoked a dose-dependent relaxation of the esophagus.
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Animal Model:Dogs[1]
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Dosage:10 and 30 μg/kg
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Administration:P.o
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Result:Produced an increase in contractility of the antrum, duodenum, and jejunum.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 916075-84-8
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Appearance Solid
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분자량 455.59
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화학식 C25H37N5O3
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Color White to light yellow
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SMILES
O=C(N1CCC(CN2CCC(CNC(C3=C4C(N=C(C(C)C)N4)=CC=C3)=O)CC2)CC1)OC
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Synonyms
TD-8954
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Naunyn Schmiedebergs Arch Pharmacol
2025 Sep 29. PMID: 41020940
용액&용해도
DMSO : 50 mg/mL (109.75 mM; ultrasonic and warming and heat to 60°C; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1950 mL | 10.9748 mL | 21.9496 mL | 54.8739 mL |
| 5 mM | 0.4390 mL | 2.1950 mL | 4.3899 mL | 10.9748 mL | |
| 10 mM | 0.2195 mL | 1.0975 mL | 2.1950 mL | 5.4874 mL | |
| 15 mM | 0.1463 mL | 0.7317 mL | 1.4633 mL | 3.6583 mL | |
| 20 mM | 0.1097 mL | 0.5487 mL | 1.0975 mL | 2.7437 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8780 mL | 2.1950 mL | |
| 30 mM | 0.0732 mL | 0.3658 mL | 0.7317 mL | 1.8291 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5487 mL | 1.3718 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0975 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9146 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6859 mL | |
| 100 mM | 0.0219 mL | 0.1097 mL | 0.2195 mL | 0.5487 mL |
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