1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Fasobegron

Fasobegron is a β3-adrenergic receptor agonist with a human EC50 of 4.8 nM. Fasobegron shows an EC50 of 250 nM for human β1-adrenergic receptors. Fasobegron can be used for the research of overactive bladder.

For research use only. We do not sell to patients.

Fasobegron

Fasobegron Chemical Structure

CAS No. : 643094-49-9

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Description

Fasobegron is a β3-adrenergic receptor agonist with a human EC50 of 4.8 nM. Fasobegron shows an EC50 of 250 nM for human β1-adrenergic receptors. Fasobegron can be used for the research of overactive bladder[1].

IC50 & Target[1]

β3 adrenoceptor

4.8 nM (EC50)

β1 adrenoceptor

250 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
>1 μM
Compound: 1a
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
[PMID: 19366244]
CHO EC50
>1 μM
Compound: 9d
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
[PMID: 18307290]
CHO EC50
250 nM
Compound: 1a
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
[PMID: 19366244]
CHO EC50
251 nM
Compound: 9d
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
[PMID: 18307290]
CHO EC50
4.8 nM
Compound: 1a
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
[PMID: 19366244]
CHO EC50
4.8 nM
Compound: 8a
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
[PMID: 18553954]
CHO EC50
4.8 nM
Compound: 9d
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
[PMID: 18307290]
In Vitro

Fasobegron (Compound 1a) potently and selectively activates human β3-ARs in CHO cells, with an EC50 of 4.8 nM, and exhibits >2000-fold selectivity over human β2-ARs (EC50 >10000 nM) and ~52-fold selectivity over human β1-ARs (EC50 = 250 nM)[1].

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

Molecular Weight

425.91

Formula

C24H24ClNO4

CAS No.
SMILES

O(C)C=1C=C(C=CC1C(O)=O)C2=CC=C(CCNC[C@H](O)C3=CC(Cl)=CC=C3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • 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.

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Fasobegron
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HY-14767
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