| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Felcisetrag contracts guinea pig colonic longitudinal muscle/myenteric plexus preparations (pEC50 = 8.6) and elevates cAMP in HEK-293 cells expressing h5-HT4(c) receptors (pEC50 = 9.3). In vitro tests reveal that felcisetrag has a moderate intrinsic action [1].
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| ln Vivo |
Felcisetrag (0.03~3 mg/kg; subcutaneous injection) shortens the time needed for carmine dye excretion and accelerates its intestinal transit [1]. The esophagus relaxes in response to felcisetrag (0.03~10 mg/kg; administered intraduodenally) in a dose-dependent manner [1]. Felcisetrag (10 and 30 μg/kg; oral) improves the duodenum, jejunum, and gastric antrum's contractility [1].
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| Animal Protocol |
Animal/Disease Models: guinea pig [1]
Doses: 0.03~3 mg/kg Route of Administration: subcutaneous injection Experimental Results: Increased colonic transport of carmine dye and shortened its excretion time. Animal/Disease Models: Rat[1] Doses: 0.03~10 mg/kg Route of Administration: Intraduodenal administration Experimental Results: Caused dose-dependent relaxation of esophagus. Animal/Disease Models: Dog [1] Doses: 10 and 30 μg/kg Route of Administration: Po Experimental Results: Increased contractility in the gastric antrum, duodenum and jejunum. |
| References |
[1]. Beattie DT, et al. The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011;2:25.
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| Additional Infomation |
Felcisetrag (TD-8954) has been used in trials studying the treatment of Enteral Feeding Intolerance and Gastrointestinal Motility Disorder.
Felcisetrag is a serotonin (5-HT) type 4 receptor agonist with potential gastrointestinal (GI) prokinetic activity. Upon administration, felcisetrag targets and binds to 5-HT4, thereby enhancing its activity. This may enhance GI motility, decrease GI tract and colonic transit time and improve constipation. |
| Molecular Formula |
C25H37N5O3
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|---|---|
| Molecular Weight |
455.603
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| Exact Mass |
455.289
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| CAS # |
916075-84-8
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| PubChem CID |
11961293
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
691.6±25.0 °C at 760 mmHg
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| Flash Point |
372.0±23.2 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.581
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| LogP |
2.34
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
658
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C(N1CCC(CC1)CN1CCC(CNC(C2=CC=CC3=C2N=C(C(C)C)N3)=O)CC1)=O
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| InChi Key |
MZOITCJKGUIQEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H37N5O3/c1-17(2)23-27-21-6-4-5-20(22(21)28-23)24(31)26-15-18-7-11-29(12-8-18)16-19-9-13-30(14-10-19)25(32)33-3/h4-6,17-19H,7-16H2,1-3H3,(H,26,31)(H,27,28)
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| Chemical Name |
methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylate
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| Synonyms |
TD 8954; TD8954; TD-8954
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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 (~109.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.49 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 25.0 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: ≥ 2.5 mg/mL (5.49 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1949 mL | 10.9745 mL | 21.9491 mL | |
| 5 mM | 0.4390 mL | 2.1949 mL | 4.3898 mL | |
| 10 mM | 0.2195 mL | 1.0975 mL | 2.1949 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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