PF-00277343
PF-00277343 is a selective and skin-penetrable THR-β (Ki: 0.51 nM for THR-β, 8.0 nM for THR-α) agonist. PF-00277343 is effective against androgenetic alopecia in animal models.
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- CAS. Nr.: 332926-04-2
- Formel: C24H20FN3O4
- Molecular Weight:433.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
0.5 nM
Compound: 5, PF-00277343
|
Binding affinity to thyroid hormone receptor in human HepG2 cells
Binding affinity to thyroid hormone receptor in human HepG2 cells
|
[PMID: 19900809] |
In Vitro
PF-00277343 is rapidly metabolized in rat liver microsomes (HLM t1/2 = 40 min), in rat hepatocytes, its half-life
is 45 min, clearance CLblood is 51 mL/min/kg and CLint is 149 mL/min/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
PF-00277343 (i.v., 0.5 mg/kg) shows thhe mean systemic plasma clearance of 40 mL/min/kg, the mean apparent volume of distribution at steady state of 4.88 mL/min/kg, and the mean terminal phase half-life of 2.73 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 332926-04-2
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Molecular Weight 433.43
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Formel C24H20FN3O4
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SMILES
O=C(N(N=C1)C2=CC(C)=C(C(C)=C2)OC3=CC=C(C(CC4=CC=C(C=C4)F)=C3)O)NC1=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)