1. Metabolic Enzyme/Protease
  2. Acetyl-CoA Carboxylase
  3. PF-05221304

PF-05221304 

Cat. No.: HY-137846 Purity: 99.43%
Handling Instructions

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polypeptides. PF-05221304 directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors.

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

PF-05221304 Chemical Structure

PF-05221304 Chemical Structure

CAS No. : 1370448-25-1

Size Price Stock Quantity
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polypeptides. PF-05221304 directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors[1].

IC50 & Target

IC50: 7.5 nM (ACC1 (rat)), 8.2 nM(ACC2 (rat)), 12.4 nM (ACC1 (human)), 8.7 nM (ACC2 (human)) [1]

In Vitro

PF-05221304 inhibits hepatic de novo lipogenesis (DNL) with an IC50 of 61 nM in human hepatocytes (donor HH AA 508) in a concentration-dependent manner. PF-05221304 stimulates fatty acid oxidation and reduces triglyceride accumulation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-05221304 treatment (5 mg/kg; oral administration; twice a day; 6 weeks) reduces the expression of these genes (a-SMA, Col1A1, Col3A1, CCL2 and CCL11), which increases by pre-treatment with choline-deficient and high-fat diet (CDAHFD). It shows chronic administration of PF-05221304 decreases hepatic inflammation and fibrosis in choline-deficient and high-fat diet-fed rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar Han rats[1]
Dosage: 5 mg/kg
Administration: Oral administration; twice a day; 6 weeks
Result: PF-05221304 treatment reduced the expression of these genes (a-SMA, Col1A1, Col3A1, CCL2 and CCL11) by 46% (P <0.01), 40% (P < 0.01), 44% (P < 0.05), 61% (P < .001) and 45% (P < .05), respectively.
Molecular Weight

502.56

Formula

C₂₈H₃₀N₄O₅

CAS No.

1370448-25-1

SMILES

O=C(O)C1=CC=C(C2=NC(OC)=CC(C(N3CCC(C4)(CC3)CC5=C(N(C(C)C)N=C5)C4=O)=O)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (198.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9898 mL 9.9491 mL 19.8981 mL
5 mM 0.3980 mL 1.9898 mL 3.9796 mL
10 mM 0.1990 mL 0.9949 mL 1.9898 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-05221304PF05221304PF 05221304Acetyl-CoA CarboxylaseACC, Acetyl Coenzyme A Carboxylaseliver-directedACChepaticInhibitorinhibitorinhibit

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Product Name:
PF-05221304
Cat. No.:
HY-137846
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