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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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Fòrmula: C₁₉H₂₂FN₅O₃S
Peso molecular:419.47

Almacenamiento:

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

GPR43 agonist 1 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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- IC₅₀ & Target
- In Vitro
- In Vivo
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Actividad biológica

Descripciòn

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^[1].

IC₅₀ & Target

^[1]

GPR43

Ver todos los productos específicos de isoformas Free Fatty Acid Receptor :

Ver todos los productos específicos de isoformas NF-κB :

In Vitro

OthersInnate ImmunityCytokines & Chemokines

Others

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].

Innate Immunity

Cytokines & Chemokines

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

Innate Immunity

GPR43 agonist 1 (30 mg/kg; p.o.; daily; 8 days) reduces colon myeloperoxidase staining but does not significantly improve clinical activity metrics or colon length in a mouse model of DSS-induced acute colitis^[1].

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

Animal Model:

C57BL/6 (female, 6 weeks old post-acclimation)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; daily; 8 days
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.

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Chemical Information

Peso molecular 419.47
Fòrmula C₁₉H₂₂FN₅O₃S
SMILES

NC1=C(S(=O)(C2=CC=CC=C2F)=O)C3=NC(C)=NC(N4C[C@@H](C)O[C@@H](C)C4)=C3N1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Park BO, et al. Novel GPR43 Agonists Exert an Anti-Inflammatory Effect in a Colitis Model. Biomolecules & therapeutics. 2022 Jan 01;30(1):48-54. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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GPR43 agonist 1

Ver todos los productos específicos de isoformas Free Fatty Acid Receptor

Ver todos los productos específicos de isoformas NF-κB