SSTR5 antagonist 4
SSTR5 antagonist 4 (compound 1) is a potent, selective and orally active somatostatin subtype 5 (SSTR5) antagonist (hSSTR5 IC50 = 1.3 nM, mSSTR5 IC50 = 1.0 nM). SSTR5 antagonist 4 shows efficacy in mouse oral glucose tolerance test (OGTT) in high fat diet (HFD)-mice. SSTR5 antagonist 4 can be used for type 2 diabetes research.
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- CAS No.: 916338-03-9
- Formule: C29H34FN3O3
- Masse moléculaire:491.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
hsst5 1.3 nM (IC50) |
mSSTR5 1.0 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>1 μM
Compound: 2Ai
|
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
|
[PMID: 20580234] |
| CHO | EC50 |
1 μM
Compound: 2Ai
|
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
|
[PMID: 20580234] |
Chemical Information
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CAS No. 916338-03-9
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Masse moléculaire 491.61
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Formule C29H34FN3O3
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SMILES
O=C(NC1CCN(CC2=CC(OCC)=C(C(OCC)=C2)C=3C=CC(F)=CC3)CC1)C4=CN=CC(=C4)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)