CGP 12177 hydrochlorideA β1/β2-AR adrenoreceptor agonist

CGP 12177 hydrochloride (CAS 81047-99-6)

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Synonym: 4-[3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one hydrochloride
Application: A β1/β2-AR adrenoreceptor agonist
CAS Number: 81047-99-6
Molecular Weight: 315.8
Molecular Formula: C14H22ClN3O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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CGP 12177 hydrochloride is a β1-AR and β2-AR adrenoreceptor antagonist. Also behaves non-conventionally as a β3-AR partial agonist.


References

Staehelin et al (1983) CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells. J.Biol.Chem. 258 3496. Strosberg and Pietri-Rouxel (1996) Function and regulation of the b3-adrenoceptor. TiPS 17 373. Galitzky et al (1998) On the presence of a putative fourth b-adrenoceptor in human adipose tissue. TiPS 19 164. Preitner et al (1998) Metabolic response to various b-adrenoceptor agonists in b3-adrenoceptor knockout mice: evidence for a new b-adrenergic receptor in brown adipose tissue. Br.J.Pharmacol. 124 1684.

Physical State :
Solid
Solubility :
Soluble in water (50 mM), and DMSO (>10 mg/ml).
Storage :
Store at room temperature
Melting Point :
258-260° C
Refractive Index :
n20D ~1.55 (Predicted)
IC50 :
β3-AR: EC5050 = 2 µM (human)
Ki Data :
β1-AR: Ki= 0.9 nM; β2-AR : Ki= 4 nM; β3-AR: Ki= 88 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
DE2565000
PubChem CID :
11957517
MDL Number :
MFCD00069230
SMILES :
CC(C)(C)NCC(COC1=CC=CC2=C1NC(=O)N2)O.Cl

Download SDS (MSDS)

Certificate of Analysis

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