GPR43 agonist 1
GPR43 agonist 1 is a selective, orally active GPR43 agonist. GPR43 agonist 1 downregulates the activity of NF-κB. GPR43 agonist 1 can be used in studies of acute colitis.
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- Formule: C19H22FN5O3S
- Masse moléculaire:419.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
GPR43 |
In Vitro
GPR43 agonist 1 (Compound 187) selectively inhibits cAMP production in HEK293-hGPR43 cells, with an EC50 value of 16 nM[1].
GPR43 agonist 1 is a potent positive allosteric agonist that induces Ca2+ influx in HEK293-hGPR43 cells, with enhanced potency in the presence of acetic acid[1].
GPR43 agonist 1 (treated for 25 min, incubated for 1 h) acts as a partial positive allosteric agonist, which induces the GPR43-β-arrestin 2 interaction in HEK293-hGPR43 cells, with enhanced activity in the presence of acetate[1].
GPR43 agonist 1 (pretreated for 20 min and co-incubated with 10 ng/mL TNF-α for 6 h) potently inhibits TNF-α-induced NF-κB activity in HEK293-hGPR43 cells, with an EC50 of 19 nM[1].
GPR43 agonist 1 reverses TNF-α-induced IκBα degradation in HEK293-hGPR43 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6 weeks old post-acclimation)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 8 days
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Result:Reduced myeloperoxidase (MPO) staining in colon tissue compared to vehicle-treated DSS-induced colitis mice.
Showed no significant change in colon length relative to vehicle-treated mice.
Reported no significant reductions in body weight loss score, rectal bleeding score, stool consistency score, or daily activity index relative to vehicle-treated mice.
Chemical Information
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Masse moléculaire 419.47
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Formule C19H22FN5O3S
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SMILES
NC1=C(S(=O)(C2=CC=CC=C2F)=O)C3=NC(C)=NC(N4C[C@@H](C)O[C@@H](C)C4)=C3N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPR43 agonist 1 Related Classifications
HY-184925 Related Classifications
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