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Art. -Nr.: HY-156259

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PF-07202954

Name: PF-07202954
Brand: MedChemExpress
SKU: HY-156259
Price: 233.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.82%
CAS. Nr.: 2639372-47-5
Formel: C₂₂H₂₃FN₆O₃
Molecular Weight:438.45

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-07202954 Chemical Structure

CAS. Nr.: 2639372-47-5

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Acyltransferase Isoform-spezifische Produkte anzeigen :

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.

Parmacokinetics

Species	Dose	Route	CL	CL_renal	V_ss	T_1/2
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.

Related Protocols :

RNA extraction experimental

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS. Nr. 2639372-47-5
Appearance Solid
Molecular Weight 438.45
Formel C₂₂H₂₃FN₆O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2808 mL

11.4038 mL

22.8076 mL

5 mM

0.4562 mL

2.2808 mL

4.5615 mL

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Filipski KJ, et al. Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life. ACS Med Chem Lett. 2023;14(10):1427-1433. Published 2023 Oct 2. [Content Brief]

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.

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.4562 mL	2.2808 mL	4.5615 mL	11.4038 mL

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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PF-07202954

Alle Acyltransferase Isoform-spezifische Produkte anzeigen