| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Felcisetrag targets the human 5-HT4(c) receptor, a G protein-coupled receptor that mediates excitatory neurotransmission in the gastrointestinal tract. It acts as a potent and selective agonist at this receptor, showing high affinity with a pKi of 9.4. Activation of the 5-HT4 receptor stimulates adenylate cyclase activity, leading to increased cyclic AMP (cAMP) levels, which in turn promotes gastrointestinal smooth muscle relaxation and propulsive motility.
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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].
In vitro, Felcisetrag produces an elevation of cAMP in HEK-293 cells expressing the human 5-HT4(c) receptor with a pEC50 of 9.3. It also contracts the guinea pig colonic longitudinal muscle/myenteric plexus preparation with a pEC50 of 8.6. The compound demonstrates moderate intrinsic activity in these in vitro assays, confirming its potent and selective agonism at the 5-HT4 receptor. |
| 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].
In vivo, Felcisetrag increases colonic transit in animal models. Subcutaneous administration at 0.03–3 mg/kg reduces the time taken for excretion of carmine red dye. Intraduodenal administration at 0.03–10 mg/kg evokes a dose-dependent relaxation of the esophagus. Oral administration at 10 and 30 μg/kg produces an increase in contractility of the antrum, duodenum, and jejunum, demonstrating its gastrointestinal prokinetic effects across multiple GI segments. |
| Enzyme Assay |
In vitro receptor binding assays for Felcisetrag measure its affinity for the human 5-HT4(c) receptor using radioligand displacement techniques. Membranes prepared from cells expressing the receptor are incubated with a radiolabeled 5-HT4 ligand and varying concentrations of the compound. The binding affinity (pKi = 9.4) is calculated from competitive binding curves. Functional assays measure receptor activation via cAMP accumulation in HEK-293 cells expressing the h5-HT4(c) receptor, with a pEC50 of 9.3.
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| Cell Assay |
In vitro cell-based assays for Felcisetrag use HEK-293 cells expressing the human 5-HT4(c) receptor. Cells are treated with serial dilutions of the compound, and intracellular cAMP levels are quantified using ELISA or other immunoassay methods. The EC50 for receptor activation is calculated from dose-response curves (pEC50 = 9.3). Functional activity in native tissue is assessed using the guinea pig colonic longitudinal muscle/myenteric plexus preparation, where contractile responses are measured (pEC50 = 8.6).
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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. In vivo animal models for Felcisetrag include guinea pig and rat models of gastrointestinal motility. Colonic transit is assessed by administering carmine red dye and measuring the time to excretion following subcutaneous administration of Felcisetrag (0.03–3 mg/kg). Esophageal relaxation is evaluated following intraduodenal administration (0.03–10 mg/kg). Gastrointestinal contractility is measured in the antrum, duodenum, and jejunum following oral administration (10 and 30 μg/kg). |
| ADME/Pharmacokinetics |
Felcisetrag is orally bioavailable and is administered via oral, subcutaneous, or intraduodenal routes in preclinical studies. The compound has a molecular weight of 455.59 and a molecular formula of C25H37N5O3. It is stored as a powder at -20°C for up to 3 years or in solution at -80°C for up to 6 months. Detailed pharmacokinetic parameters including half-life, clearance, and bioavailability are documented in research publications.
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| Toxicity/Toxicokinetics |
The toxicity profile of Felcisetrag has been characterized in preclinical safety studies. As a 5-HT4 receptor agonist, the compound is generally well-tolerated at therapeutic doses. Common adverse effects may include gastrointestinal discomfort. The compound's safety margin and no-observed-adverse-effect level (NOAEL) are documented in regulatory submissions. The compound is for research use only and not for human use.
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| 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 |
Fecilevir (TD-8954) has been investigated for the treatment of enteral nutrition intolerance and gastrointestinal motility disorders. Fecilevir is a 5-hydroxytryptamine (5-HT) type 4 receptor agonist with potential gastrointestinal (GI) prokinetic effects. After administration, fecitrevir targets and binds to the 5-HT4 receptor, thereby enhancing its activity. This may enhance gastrointestinal motility, shorten transit time in the gastrointestinal tract and colon, and improve constipation.
Felcisetrag (TD-8954) is a research compound that has been used in clinical trials studying the treatment of enteral feeding intolerance and gastrointestinal motility disorder. It is also known by the synonyms TD-8954 and THRX-149699. The compound's high affinity (pKi = 9.4) for the human 5-HT4(c) receptor makes it a valuable tool for studying 5-HT4 receptor pharmacology and gastrointestinal motility. It is not approved for clinical use and is intended for research purposes only. |
| 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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