2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. β3-AR agonist 1

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

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β3-AR agonist 1

β3-AR agonist 1 Estructura química

No. CAS : 1283125-73-4

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β3-AR agonist 1 Related Antibodies

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Descripciòn

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1].

IC50 & Target

EC50: 18 nM (β3-AR)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 10000 nM
Compound: 15
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
[PMID: 28355078]
HEK293 EC50
> 10000 nM
Compound: 15
Agonist activity at recombinant human alpha1B adrenergic receptor expressed in HEK293 cells after 6 hrs by NFAT-luciferase reporter gene assay
Agonist activity at recombinant human alpha1B adrenergic receptor expressed in HEK293 cells after 6 hrs by NFAT-luciferase reporter gene assay
[PMID: 28355078]
HEK293 EC50
> 10000 nM
Compound: 15
Agonist activity at recombinant human alpha1D adrenergic receptor expressed in HEK293 cells after 6 hrs by NFAT-luciferase reporter gene assay
Agonist activity at recombinant human alpha1D adrenergic receptor expressed in HEK293 cells after 6 hrs by NFAT-luciferase reporter gene assay
[PMID: 28355078]
In Vivo

β3-AR agonist 1 (compound 15) shows dose-dependent β3-AR-mediated responses in marmoset urinary bladder smooth muscle, has a desirable metabolic stability and pharmacokinetic profile (Cmax and AUC), and do not obviously affect heart rate or mean blood pressure when administered intravenously (3 mg/kg) to anesthetized rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Peso molecular

444.55

Fòrmula

C22H28N4O4S
No. CAS
SMILES

O=S(NC1=CC([C@@H](O)CNCCOC2=CC(NN=C3C)=C3C=C2)=CC=C1)(C4CCC4)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
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β3-AR agonist 1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

β3-AR agonist 11283125-73-4Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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