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AZ13581837

Chemical Structure : AZ13581837

CAS No.: 2896777-27-6

AZ13581837 (AZ 13581837)

Catalog No.: PC-20425Not For Human Use, Lab Use Only.

AZ13581837 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 5.2 nM and 4.3 nM for stimulation of DMR response in CHO-hGPR120/mGPR120 cells, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZ13581837 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 5.2 nM and 4.3 nM for stimulation of DMR response in CHO-hGPR120/mGPR120 cells, respectively.
AZ13581837 has IC50 of 120 nM calcium mobilization assays, does not activate mouse GPR40 in a calcium mobilization assay.
AZ13581837 is about 100-fold more potent than Metabolex-36, AZ13581837 is selective for human and mouse GPR120 without activity on GPR40.
AZ13581837 selectively induces a calcium response in CHO-hGPR120 cells with EC50 of 120 nM, induces GPR120 dependent calcium mobilization, DMR response and cAMP production in GPR120 overexpressing cells.
AZ13581837 (10 uM) inhibits cAMP production in mouse islets and increase GLP-1 secretion from STC-1 cells.
AZ13581837 (18 mg/kg) improve oral glucose tolerance, increases insulin secretion in IVGTT in lean mice.

Physicochemical Properties

M.Wt 362.40
Formula C20H14N2O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(3-ethynyl-5-(3-pyridyloxy)phenyl)-3H-1,2-benzothiazole 1,1-dioxide

References

1. Sundström L, et al. PLoS One. 2017 Dec 5;12(12):e0189060.

2. Marine L Croze, et al. Mol Metab. 2021 Mar;45:101166.

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