957136-80-0
Chemical Structure
GIV3727
- CAS No.: 957136-80-0
- Formula:C12H22O2
- Molecular Weight:198.30
IUPAC Name: 4-(2,2,3-trimethylcyclopentyl)butanoic acid
InChIKey: LYFXCRCUENNESS-UHFFFAOYSA-N
SMILES: OC(CCCC1CCC(C1(C)C)C)=O
Biological Activity: GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research[1][2].
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GIV3727 | GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research. | |||||||||||||||||||||
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References
- [1]. Wang Q, et al. Bitter-tasting drugs tune GDF15 and GLP-1 expression via bitter taste or motilin receptors in the intestine of patients with obesity. Molecular metabolism. 2024 Oct;88:102002.
- [2]. Slack JP, et al. Modulation of bitter taste perception by a small molecule hTAS2R antagonist. Current biology : CB. 2010 Jun 22;20(12):1104-9. [Content Brief]
