PF-429242

Name: PF-429242
Brand: MedChemExpress
SKU: HY-13447
Rating: 5.0 (10 reviews)

Cat. No.: HY-13447 Purity: 99.59%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

PF429242 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.

CAS No. : 947303-87-9

Size	Stock	Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Oil
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of PF-429242:

PF429242 dihydrochloride In-stock

10 Publications Citing Use of MCE PF-429242

Cell Imaging/Staining

ELISA

Histological Imaging/Staining

: PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]; PF429242 dihydrochloride (5-10 μM) significantly inhibited osteoclasts formation in murine BMMs in a dose-dependent manner.

: PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]; PF429242 dihydrochloride (3 mg/kg; twice a week for 2 months) significantly increased the values of BV/TV and decreased Tb.Sp in OVX-induced osteoporosis mice.

: PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]; PF429242 dihydrochloride (3 mg/kg; every two days for 2 weeks) reduced osteolysis and osteoclast activity in LPS-induced calvarial osteolysis mice.

: PF-429242 purchased from MedChemExpress. Usage Cited in: Immunity. 2018 Nov 20;49(5):842-856.e7. [Abstract]; PF429242 dihydrochloride (50-200 μM; 1 h) greatly suppressed the NLRP3 inflammasome activity in LPS-primed BMDMs.

: PF-429242 purchased from MedChemExpress. Usage Cited in: Immunity. 2018 Nov 20;49(5):842-856.e7. [Abstract]; PF429242 dihydrochloride (200 μM; 1 h) suppressed nigericin-induced SREBP2 maturation in LPS-primed THP1 macrophages.

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Biological Activity
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References
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Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	170 nM Compound: 1u, PF-429242	Inhibition of human S1P expressed in CHOK1 cells Inhibition of human S1P expressed in CHOK1 cells	[PMID: 17583500]
HepG2	EC₅₀	600 nM Compound: 1u, PF-429242	Inhibition of cholesterol synthesis in HepG2 cells Inhibition of cholesterol synthesis in HepG2 cells	[PMID: 17583500]
Hepatocyte	EC₅₀	0.3 μM Compound: 1u, PF-429242	Reduction of HMG-CoA synthase expression in mouse hepatocytes Reduction of HMG-CoA synthase expression in mouse hepatocytes	[PMID: 17583500]
Hepatocyte	EC₅₀	2 μM Compound: 1u, PF-429242	Reduction of fatty acid synthase expression in mouse hepatocytes Reduction of fatty acid synthase expression in mouse hepatocytes	[PMID: 17583500]

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

409.56

Formula

C₂₅H₃₅N₃O₂

CAS No.

947303-87-9

Appearance

Oil

Color

Colorless to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (61.04 mM; Need ultrasonic; 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	2.4416 mL	12.2082 mL	24.4164 mL
5 mM	0.4883 mL	2.4416 mL	4.8833 mL
10 mM	0.2442 mL	1.2208 mL	2.4416 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.

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 (6.10 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 (6.10 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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.59%

Select Batch:

Data Sheet (274 KB) SDS (537 KB)

COA (247 KB) HNMR (435 KB) RP-HPLC (257 KB) LCMS (97 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 Exp Ther. 2008 Sep;326(3):801-8. [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. [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

DMSO	1 mM	2.4416 mL	12.2082 mL	24.4164 mL	61.0411 mL
	5 mM	0.4883 mL	2.4416 mL	4.8833 mL	12.2082 mL
	10 mM	0.2442 mL	1.2208 mL	2.4416 mL	6.1041 mL
	15 mM	0.1628 mL	0.8139 mL	1.6278 mL	4.0694 mL
	20 mM	0.1221 mL	0.6104 mL	1.2208 mL	3.0521 mL
	25 mM	0.0977 mL	0.4883 mL	0.9767 mL	2.4416 mL
	30 mM	0.0814 mL	0.4069 mL	0.8139 mL	2.0347 mL
	40 mM	0.0610 mL	0.3052 mL	0.6104 mL	1.5260 mL
	50 mM	0.0488 mL	0.2442 mL	0.4883 mL	1.2208 mL
	60 mM	0.0407 mL	0.2035 mL	0.4069 mL	1.0174 mL

PF-429242 Related Classifications

Metabolic Disease Infection

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-429242947303-87-9PF429242PF 429242Fatty Acid Synthase (FASN)Virus ProteaseInhibitorinhibitorinhibit

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PF-429242

Customer Review

Other Forms of PF-429242:

PF-429242 Related Antibodies

10 Publications Citing Use of MCE PF-429242

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

PF-429242 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

PF-429242 Related Classifications

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