2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. PF-07202954

PF-07202954 is an orally active, highly selective DGAT2 inhibitor with an IC50 of 10 nM against human DGAT2 and an IC50 of 17 nM against rat DGAT2. PF-07202954 reduces triglyceride synthesis, decreases hepatic triglyceride content and plasma triglyceride levels, inhibits de novo lipogenesis, and suppresses the hepatic SREBP signaling pathway as well as the expression of SREBP target genes. PF-07202954 is applicable to research related to non-alcoholic steatohepatitis.

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

PF-07202954

PF-07202954 Chemical Structure

CAS No. : 2639372-47-5

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PF-07202954 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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Description

PF-07202954 is an orally active, highly selective DGAT2 inhibitor with an IC50 of 10 nM against human DGAT2 and an IC50 of 17 nM against rat DGAT2. PF-07202954 reduces triglyceride synthesis, decreases hepatic triglyceride content and plasma triglyceride levels, inhibits de novo lipogenesis, and suppresses the hepatic SREBP signaling pathway as well as the expression of SREBP target genes. PF-07202954 is applicable to research related to non-alcoholic steatohepatitis[1].

In Vitro

PF-07202954 inhibits DGAT2-mediated triglyceride synthesis in cryopreserved human hepatocytes with an IC50 of 11 nM[1].

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

PF-07202954 Related Antibodies
Parmacokinetics
Species Dose Route CL CLrenal Vss T1/2
Rat[1] 1 mg/kg i.v. 64 mL/min/kg 7.5 mL/min/kg 2.7 L/kg 0.9 h
Monkey[1] 1 mg/kg i.v. 17 mL/min/kg 0.29 mL/min/kg 1.6 L/kg 1.4 h
Dog[1] 1 mg/kg i.v. 22 mL/min/kg 5.5 mL/min/kg 2.1 L/kg 1.5 h
In Vivo

PF-07202954 (3-100 mg/kg; p.o.; twice daily; for 8 consecutive days) reduces plasma and hepatic triglyceride levels in Western diet-fed rats in a dose-dependent manner[1].

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

Animal Model: Western-diet-fed rats
[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; twice daily; 8 days
Result: Reduced plasma triglycerides.
Reduced liver triglycerides.
Achieved a 71% reduction in plasma triglycerides at 100 mg/kg dose.
Achieved a 48% reduction in liver triglycerides at 100 mg/kg dose.
Reduced multiple SREBP target genes in a dose-dependent manner.
Clinical Trial
Molecular Weight

438.45

Formula

C22H23FN6O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CN=C(C2=CC(OC3=NC=CC=C3OCC)=CN=C2)N=C1)N[C@@H]4CNC[C@@H](F)C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (7.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2808 mL 11.4038 mL 22.8076 mL
5 mM 0.4562 mL 2.2808 mL 4.5615 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.82% ee.: 100.00%

SDS (251 KB)

COA (247 KB) HNMR (298 KB) NP-HPLC (279 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2808 mL 11.4038 mL 22.8076 mL 57.0190 mL
5 mM 0.4562 mL 2.2808 mL 4.5615 mL 11.4038 mL
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PF-07202954 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

PF-072029542639372-47-5PF07202954PF 07202954AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT2rat DGAT2non-alcoholic steatohepatitisplasma triglyceride levelscryopreserved human hepatocyteshuman DGAT2triglyceride synthesisde novo lipogenesishepatic SREBP signalingliver triglyceride contentInhibitorinhibitorinhibit

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