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.
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- CAS No.: 2768029-03-2
- 화학식: C11H7Cl2N3S2
- 분자량:316.23
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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) 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.
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Animal Model:Gastrointestinal motility model established in male CD-1 mice (6 weeks old)[1]
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Dosage:1, 10, and 100 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Significantly increased the defecation volume, fecal weight and fecal moisture content of the mice at 100 mg/kg.
No obvious abnormalities were observed in the mice regarding their movement, behavior, or general health conditions.
Chemical Information
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CAS No. 2768029-03-2
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분자량 316.23
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화학식 C11H7Cl2N3S2
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SMILES
ClC1=CN=C(CNC2=CC3=C(C=C2Cl)C=NS3)S1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRPM5 agonist-1 Related Classifications
HY-178236 Related Classifications
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