PF429242 dihydrochloride

Name: PF429242 dihydrochloride
Brand: MedChemExpress
SKU: HY-13447A
Rating: 5.0 (7 reviews)

Cat. No.: HY-13447A Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC₅₀ of 175 nM.

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

PF429242 dihydrochloride Chemical Structure

CAS No. : 2248666-66-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 117	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 117	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of PF429242 dihydrochloride:

PF-429242 Get quote

7 Publications Citing Use of MCE PF429242 dihydrochloride

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC₅₀ of 175 nM^[1].

IC₅₀ & Target

IC50: 175 nM (S1P)^[1]

In Vitro

10 μM PF-429242 inhibits endogenous SREBP processing in Chinese hamster ovary cells. PF-429242 also down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In HepG2 cells, PF-429242 inhibits cholesterol synthesis, with an IC₅₀ of 0.5 μM^[1]. The addition of PF-429242 (30 μM) shows statistically significant suppression of infectious viral titers and viral RNA copies in the cell culture fluids. PF-429242 treatment also shows suppressive effects on DENV2 yields in the cultured fluids of human-derived HEK-293, Hep G2, and non-human-primate derived LLC-MK2 cells^[2]. PF-429242 efficiently prevents the processing of GPC from the prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV, which correlates with the compound's potent antiviral activity against LCMV and LASV in cultured cells^[3].

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

In Vivo

In mice treated with PF-429242 for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced^[1].

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

Molecular Weight

482.49

Formula

C₂₅H₃₇Cl₂N₃O₂

CAS No.

2248666-66-0

Appearance

Solid

Color

White to light brown

SMILES

O=C(N(CCC1=CC=CC=C1OC)[C@H]2CNCC2)C3=CC=C(CN(CC)CC)C=C3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 83.3 mg/mL (172.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (103.63 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0726 mL	10.3629 mL	20.7258 mL
5 mM	0.4145 mL	2.0726 mL	4.1452 mL
10 mM	0.2073 mL	1.0363 mL	2.0726 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (207.26 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (249 KB) HNMR (309 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol [Content Brief]

[2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046. [Content Brief]

[3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803. [Content Brief]

Animal Administration
^[1]

Mice: To test the in vivo efficacy of PF-429242 in regulating SREBP target genes, male CD1 mice are dosed i.p. with 10 or 30 mg/kg PF-429242 or saline once every 6 over a 24-h period. Mice are euthanized 6 h after the final dose, and liver tissue is collected, frozen rapidly in liquid nitrogen, and stored at -80°C. For RNA isolation, 50 to 100 mg of frozen liver tissue from each sample is homogenized in 1 ml of TRIzol reagent. Total RNA is extracted following the manufacturer's instructions, and the resulting total RNA from each sample underwent DNA-free treatment^[1].

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

References

[1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol [Content Brief]

[2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046. [Content Brief]

[3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.0726 mL	10.3629 mL	20.7258 mL	51.8145 mL
	5 mM	0.4145 mL	2.0726 mL	4.1452 mL	10.3629 mL
	10 mM	0.2073 mL	1.0363 mL	2.0726 mL	5.1815 mL
	15 mM	0.1382 mL	0.6909 mL	1.3817 mL	3.4543 mL
	20 mM	0.1036 mL	0.5181 mL	1.0363 mL	2.5907 mL
	25 mM	0.0829 mL	0.4145 mL	0.8290 mL	2.0726 mL
	30 mM	0.0691 mL	0.3454 mL	0.6909 mL	1.7272 mL
	40 mM	0.0518 mL	0.2591 mL	0.5181 mL	1.2954 mL
	50 mM	0.0415 mL	0.2073 mL	0.4145 mL	1.0363 mL
	60 mM	0.0345 mL	0.1727 mL	0.3454 mL	0.8636 mL
	80 mM	0.0259 mL	0.1295 mL	0.2591 mL	0.6477 mL
	100 mM	0.0207 mL	0.1036 mL	0.2073 mL	0.5181 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.