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Cat. No.: HY-118978

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PF-00277343

PF-00277343 is a selective and skin-penetrable THR-β (K_i: 0.51 nM for THR-β, 8.0 nM for THR-α) agonist. PF-00277343 is effective against androgenetic alopecia in animal models.

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

CAS No.: 332926-04-2
Formula: C₂₄H₂₀FN₃O₄
Molecular Weight:433.43

Storage:

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

Data Sheet (267 KB)

PF-00277343 Chemical Structure

CAS No.: 332926-04-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PF-00277343 is a selective and skin-penetrable THR-β (K_i: 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 t_1/2 = 40 min), in rat hepatocytes, its half-life is 45 min, clearance CL_blood is 51 mL/min/kg and CL_int 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.

Chemical Information

CAS No. 332926-04-2
Molecular Weight 433.43
Formula C₂₄H₂₀FN₃O₄
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li JJ, et al. Thyroid receptor agonists for the treatment of androgenetic alopecia. Bioorg Med Chem Lett. 2010 Jan 1;20(1):306-8. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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