A GRK-biased agonist of β2-AR
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

ATR-258

Item No. 45371

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αR-[[(1,1-dimethylethyl)amino]methyl]-5-fluoro-3-pyridinemethanol
CAS Number
2301983-88-8
Molecular Formula
C11H17FN2O
Formula Weight
212.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Sparingly soluble: 1-10 mg/ml
SMILES
FC1=CC([C@H](CNC(C)(C)C)O)=CN=C1
InChi Code
InChI=1S/C11H17FN2O/c1-11(2,3)14-7-10(15)8-4-9(12)6-13-5-8/h4-6,10,14-15H,7H2,1-3H3/t10-/m0/s1
InChi Key
SASMSPQPEDQJII-JTQLQIEISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $25

    Add

    5 mg

    $113

    Add

    10 mg

    $200

    Add

    25 mg

    $438

    Add
    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    Product Description

    ATR-258 is a GRK-biased agonist of the β2-adrenergic receptor (β2-AR).1 It binds to the orthosteric site on β2-AR and mediates glucose uptake dependent on G protein-coupled receptor kinase 2 (GRK2) with low Gαs-dependent cAMP generation in a phenotypic screen. ATR-258 (10 µM) increases glucose uptake in L6 cells that endogenously express β2-AR, an effect that can be blocked by the β2-AR antagonist ICI 118551 (Item No. 15591) or the mTORC2 inhibitor JR-AB2-011. Oral administration of ATR-258 (0.3 mg/kg) improves glucose tolerance, reduces fat mass, and increases lean mass in diet-induced obese (DIO) mice without increasing heart weight. ATR-258 in combination with liraglutide (Item No. 24727) reduces fat mass without reducing lean mass in DIO mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Motso, A., Pelcman, B., Kalinovich, A., et al. GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity. Cell 188(19), 5142-5156 (2025).