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TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 value of 8.1. It displays excellent selectivity for related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4) with selectivity greater than 100-fold. TRPM5 agonist-1 induces local stimulation of gastrointestinal transit in mice and is useful for studying the promotion of gastric motility.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 value of 8.1. It displays excellent selectivity for related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4) with selectivity greater than 100-fold. TRPM5 agonist-1 induces local stimulation of gastrointestinal transit in mice and is useful for studying the promotion of gastric motility. |
| In vitro | TRPM5 agonist-1 (Compound 64) exhibits a high clearance rate in both human and mouse liver microsomes and demonstrates an extremely high plasma protein binding rate. |
| In vivo | TRPM5 agonist-1 (Compound 64), when administered orally at doses ranging from 1 to 100 mg/kg, maintains a high concentration in the intestinal target tissues of mice for an extended period, with minimal entry into systemic circulation. In mouse models, TRPM5 agonist-1 at the same dosage displays a pronounced effect on enhancing gastrointestinal motility, increasing both the frequency and weight of stools while also softening them. |
| Molecular Weight | 316.22 |
| Formula | C11H7Cl2N3S2 |
| Cas No. | 2768029-03-2 |
| Smiles | ClC=1SC(=NC1)CNC2=CC=3SN=CC3C=C2Cl |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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