TRPM5 agonist-1 

TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC₅₀ of 8.1. TRPM5 agonist-1 shows excellent selectivity (> 100-fold) versus related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4). TRPM5 agonist-1 exhibits locally acting stimulatory effect on gastrointestinal transit in mice. TRPM5 agonist-1 can be used for research on promoting gastric motility^[1].

TRPM5 agonist-1 (Compound 64) exhibits high clearance rates in both human and mouse liver microsomes, and also has a very high plasma protein binding rate^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TRPM5 agonist-1 (Compound 64) (1-100 mg/kg, p.o., single dose) concentrates in the intestinal target tissues at a high level for a long time, while rarely entering the systemic blood circulation in mice^[1].
TRPM5 agonist-1 (Compound 64) (1-100 mg/kg, p.o., single dose) demonstrates a significant gastrointestinal motility-promoting effect in the mouse model, capable of increasing the frequency of defecation and the weight of feces, while also softening the feces^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

316.23

C₁₁H₇Cl₂N₃S₂

2768029-03-2

ClC1=CN=C(CNC2=CC3=C(C=C2Cl)C=NS3)S1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Barilli A, et al. From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents. J Med Chem. 2021 May 13;64(9):5931-5955.  [Content Brief]