Aleniglipron | GLP-1R agonist | Probechem Biochemicals

Chemical Structure : Aleniglipron

CAS No.: 2685823-26-9

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Aleniglipron (GSBR-1290, GSBR1290)

货号: PC-23667Not For Human Use, Lab Use Only.

Aleniglipron (GSBR-1290) is a fully biased, orally available, potent GLP-1R agonist with binding Ki of <10 nM and cAMP EC50 of <0.1 nM.

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5 mg	￥3980	In stock
10 mg	￥5880	In stock
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生物&药学活性

Aleniglipron (GSBR-1290) is a fully biased, orally available, potent GLP-1R agonist with binding Ki of <10 nM and cAMP EC50 of <0.1 nM.
GSBR-1290 strongly activated GLP-1R Gαs cAMP pathway without inducing measurable β-arrestin recruitment signaling, which indicates it is a fully biased agonist.
GSBR-1290 showed dose dependent induction of insulin secretion
GSBR-1290 strongly induced insulin secretion and glucose clearance in acute intravenous glucose tolerance test (ivGTT).
GSBR-1290 administered orally once daily for 7-day demonstrated robust increase in insulin secretion and glucose clearance in ivGTT and a dose dependent reduction of food intake and body weight.

物理化学性质&存储条件

分子量	916.01
分子式	C49H55FN9O6P
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-((1S,2S)-1-(2-((S)-3-(3-(4-(Diethylphosphoryl)-3-(methylamino)phenyl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl)-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-5-carbonyl)-5-(tetrahydro-2H-pyran-4-yl)-1H-indol-1-yl)-2-methylcyclopropyl)-1,2,4-oxadiazol-5(4H)-one

参考文献

1. TING MAO, et al. Discovery of GSBR-1290, a Highly Potent, Orally Available, Novel Small Molecule GLP-1 Receptor Agonist, Diabetes 2023;72(Supplement_1):760-P.

Aleniglipron (GSBR-1290, GSBR1290)

生物&药学活性

物理化学性质&存储条件

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Aleniglipron (GSBR-1290, GSBR1290)

生物&药学活性

物理化学性质&存储条件

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