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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G274765-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $21.90 | |
G274765-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $88.90 | |
G274765-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $128.90 | |
G274765-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $333.90 | |
G274765-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $528.90 |
Potent, highly selective 5-HT 4 antagonist
Synonyms | AB00443520 | (1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate | GR 113808 | HY-103152 | [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate | EU-0100282 | GR-113,808 | SDCCGSBI-0050270.P0 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent, highly selective 5-HT 4 receptor antagonist (pK b = 8.8). Displays > 300-fold selectivity over 5-HT 1A , 5-HT 1B , 5-HT 2A , 5-HT 2C and 5-HT 3 receptors. Decreases water intake and potentiates drinking. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of 5-HT 4 receptor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description |
GR 113808 has been used as a serotonin receptor 4 (5-HT4R) blocker to investigate its effect on calcium (Ca2+) transients in rat ventricular cardiomyocytes. It has also been used as a 5-HT4R antagonist to study its effects on nebogenesis in post-embryonic zebrafish
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate |
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INCHI | InChI=1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3 |
InChi Key | MOZPSIXKYJUTKI-UHFFFAOYSA-N |
Canonical SMILES | CN1C=C(C2=CC=CC=C21)C(=O)OCC3CCN(CC3)CCNS(=O)(=O)C |
Isomeric SMILES | CN1C=C(C2=CC=CC=C21)C(=O)OCC3CCN(CC3)CCNS(=O)(=O)C |
Alternate CAS | 144625-51-4 |
PubChem CID | 119376 |
MeSH Entry Terms | (1-(2-(methylsulfonylamino)ethyl)-4-piperidinyl)methyl 1-methyl-1H-indole-3-carboxylate;GR 113808;GR 125487;GR-113808;GR113808 |
Molecular Weight | 393.50 |
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Solubility | Soluble in DMSO to 100 mM and in ethanol to 10 mM |
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Sensitivity | Moisture Sensitive |