A β1-AR antagonist
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CGP 20712A

Item No. 40765

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy]propyl]amino]ethoxy]-benzamide, monomethanesulfonate
CAS Number
105737-62-0
Molecular Formula
C23H25F3N4O5 • CH3SO3H
Formula Weight
590.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1mg/mlDMSO: Sparingly Soluble: 1-10 mg/mlMethanol: Slightly Soluble: 0.1-1mg/ml
SMILES
O=C(C1=CC(OCCNCC(COC2=CC=C(C3=NC(C(F)(F)F)=CN3C)C=C2)O)=CC=C1O)N.O=S(O)(C)=O
InChi Code
InChI=1S/C23H25F3N4O5.CH4O3S/c1-30-12-20(23(24,25)26)29-22(30)14-2-4-16(5-3-14)35-13-15(31)11-28-8-9-34-17-6-7-19(32)18(10-17)21(27)33;1-5(2,3)4/h2-7,10,12,15,28,31-32H,8-9,11,13H2,1H3,(H2,27,33);1H3,(H,2,3,4)
InChi Key
VFPOVCXWKBYDNF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $164

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    10 mg

    $251

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    Product Description

    CGP 20712A is an antagonist of the β1-adrenergic receptor (β1-AR; IC50 = 0.7 nM).1 It is selective for β1-ARs over β2-ARs (IC50 = 6,700 nM). CGP 20712 A (0.1-1,000 µM) inhibits adenylyl cyclase activity induced by the β1- and β2-AR agonist isoproterenol (Item No. 15592) in brown adipose tissue plasma membranes isolated from both lean and pre-obese rat pups.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dooley, D.J., Bittiger, H., and Reymann, N.C. CGP 20712 A: A useful tool for quantitating β1- and β2-adrenoceptors. Eur. J. Pharmacol. 130(1-2), 137-139 (1986).

    2. Charon, C., Krief, S., Diot-Dupuy, F., et al. Early alterations in the brown adipose tissue adenylate cyclase system of pre-obese Zucker rat fa/fa pups: Decreased G-proteins and β3-adrenoceptor activities. Biochem J. 312(Pt 3), 781-788 (1995).