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PF 429242

Katalog-Nr.GC15234

inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease

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PF 429242 Chemische Struktur

Cas No.: 947303-87-9

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Sample solution is provided at 25 µL, 10mM.

Protocol of PF 429242

Animal experiment:

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].

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.
[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.
[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.

Chemical Properties of PF 429242

Cas No. 947303-87-9 SDF
Chemical Name (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
Canonical SMILES CCN(CC1=CC=C(C(N([C@]2([H])CCNC2)CCC3=CC=CC=C3OC)=O)C=C1)CC
Formula C25H35N3O2.2HCl M.Wt 482.49
Löslichkeit <24.12mg/ml in Water; <24.12mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PF 429242

Prepare stock solution
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
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In vivo Formulation Calculator (Clear solution) of PF 429242

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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