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ATR-258

Chemical Structure : ATR-258

CAS No.: 2301983-88-8

ATR-258 (ATR258)

Catalog No.: PC-24799Not For Human Use, Lab Use Only.

ATR-258 (Compound 15) is a specific GRK-biased β2 adrenergic receptor (β2AR) agonist with pEC50 of 6.87, increases glucose uptake with low cAMP generation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ATR-258 (Compound 15) is a specific GRK-biased β2 adrenergic receptor (β2AR) agonist with pEC50 of 6.87, increases glucose uptake with low cAMP generation.
ATR-258 induces minimal internalization compared with compounds that stimulate β-arrestin recruitment.
ATR-258 acts as a competitive β1AR antagonist and shows weak partial agonist activity at β3AR at 10 μM, exhibits high selectivity in the glucose uptake assay.
ATR-258 (0.3 or 0.1 mg/kg) by daily oral gavage for 18 days promotes glucose control with reduced side effects in mouse model of diabetes, acting through GRK2 to mediate glucose uptake in skeletal muscle and improve glycemic control.
ATR-258 (10 mg/kg/day) by daily oral gavage improves muscle mass in a rodent model for diabetic muscular atrophy.

Physicochemical Properties

M.Wt 212.27
Formula C11H17FN2O
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

(R)-2-(tert-butylamino)-1-(5-fluoropyridin-3-yl)ethan-1-ol

References

1. Motso A, et al. Cell. 2025 Jun 19:S0092-8674(25)00630-0.

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