1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. 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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PF-00277343

PF-00277343 화학구조

CAS No. : 332926-04-2

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제품 설명

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[1].

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 (1 mg/mL and 0.1 mg/mL, single topical application) is effective in inducing hair growth in C3H female mice[1].
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.

분자량

433.43

화학식

C24H20FN3O4

CAS No.
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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

순도&문서
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    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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Inquiry Information

상품명:
PF-00277343
Cat. No.:
HY-118978
수량:
MCE Japan Authorized Agent: