KB-141
KB-141 is a potent and selective TRβ agonist. The IC50 values are 23.9 nM and 3.3 nM for binding affinities from displacement of T3 from hTRα1 and hTRβ1, respectively. KB-141 has anti-obesity, anti-diabetic, and lipid-lowering effects?and can be used as an anti-cholesteremic agent in vivo.
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- CAS No.: 219691-94-8
- Formule: C17H16Cl2O4
- Masse moléculaire:355.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
219691-94-8
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
0.78 nM
Compound: 2a
|
Activity against TRAFbeta expressed in CHOK1 cells by alkaline phosphatse reporter gene assay
Activity against TRAFbeta expressed in CHOK1 cells by alkaline phosphatse reporter gene assay
|
[PMID: 17543524] |
| CHO-K1 | EC50 |
1.7 nM
Compound: 2a
|
Activity against TRAF-alpha-1 expressed in CHOK1 cells by alkaline phosphatase reporter gene assay
Activity against TRAF-alpha-1 expressed in CHOK1 cells by alkaline phosphatase reporter gene assay
|
[PMID: 17543524] |
| CHO-K1 | EC50 |
11 nM
Compound: 15
|
Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined
Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined
|
[PMID: 12699376] |
| CHO-K1 | EC50 |
3.5 nM
Compound: 15
|
Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined
Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined
|
[PMID: 12699376] |
| CHO-K1 | IC50 |
1.1 nM
Compound: 2a
|
Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells
Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells
|
[PMID: 17543524] |
| CHO-K1 | IC50 |
25 nM
Compound: 2a
|
Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells
Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells
|
[PMID: 17543524] |
| CV-1 | EC50 |
1.12 nM
Compound: 2, KB-141
|
Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay
Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay
|
[PMID: 18585912] |
| CV-1 | EC50 |
4.5 nM
Compound: 2, KB-141
|
Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay
Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay
|
[PMID: 18585912] |
Chemical Information
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CAS No. 219691-94-8
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Masse moléculaire 355.21
-
Formule C17H16Cl2O4
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SMILES
O=C(CC1=CC(Cl)=C(C(Cl)=C1)OC2=CC=C(C(C(C)C)=C2)O)O
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)