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.
For research use only. We do not sell to patients.
- CAS No.: 957136-80-0
- Formula: C12H22O2
- Molecular Weight:198.30
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Storage:
Solution, -20°C, 2 years
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GDF15 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
6.4 μM
|
Inhibition of acesulfame K-induced activation of hTAS2R31 in HEK293 cells expressing hTAS2R31 and G16gust44 measured by high-throughput calcium imaging.
Inhibition of acesulfame K-induced activation of hTAS2R31 in HEK293 cells expressing hTAS2R31 and G16gust44 measured by high-throughput calcium imaging.
|
20537538 |
| HEK293 | IC50 |
7.9 μM
|
Inhibition of saccharin-induced activation of hTAS2R31 in HEK293 cells expressing hTAS2R31 and G16gust44 measured by high-throughput calcium imaging.
Inhibition of saccharin-induced activation of hTAS2R31 in HEK293 cells expressing hTAS2R31 and G16gust44 measured by high-throughput calcium imaging.
|
20537538 |
In Vitro
The TAS2R antagonist GIV3727 (110 µM; 30 min) blocks gallic acid-induced GDF15 mRNA expression in primary jejunal crypts but does not affect GLP-1 mRNA expression or azithromycin-induced GDF15 mRNA expression[1].
GIV3727 (6.4 μM; acesulfame K) is a novel, reversible antagonist of hTAS2R31, inhibiting activation by acesulfame K and saccharin with IC50 values of 6.4 μM and 7.9 μM, respectively, and also inhibits hTAS2R43[2].
GIV3727 (6-25 μM) acts as an orthosteric, insurmountable antagonist of hTAS2R31, increasing agonist EC50 3- to 10-fold and decreasing maximal signal amplitude by 35-70% at 25 μM[2].
GIV3727 (6-25 μM) significantly reduces hTAS2R31 receptor activation across all concentrations of acesulfame K, saccharin, and aristolochic acid[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 957136-80-0
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Appearance Liquid
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Molecular Weight 198.30
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Formula C12H22O2
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Color Colorless to light yellow
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SMILES
OC(CCCC1CCC(C1(C)C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Solution, -20°C, 2 years
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GIV3727 Related Classifications
HY-124956 Related Classifications
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