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PLX5622 hemifumarate

Catalog No.GC38836

El hemifumarato PLX5622 es un inhibidor de CSF1R activo por vÍa oral y penetrante en el cerebro altamente selectivo (IC50 = 0,016 μM; Ki = 5,9 nM).

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PLX5622 hemifumarate Chemical Structure

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
119,00 $
Disponible
1mg
49,00 $
Disponible
5mg
108,00 $
Disponible
10mg
176,00 $
Disponible
25mg
295,00 $
Disponible
50mg
414,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of PLX5622 hemifumarate

PLX5622 hemifumarate is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals[1][2].

PLX5622 hemifumarate (oral gavage; 65 mg/kg/day; for 14 days) causes paw withdrawal threshold high in mice, indicating that PLX5622 prevents the development of injury-associated mechanical allodynia[2]. Animal Model: C57BL/6 mice (males, 10-12 weeks old, 20-25 g)[2]

[1]. Spangenberg E, et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758. [2]. Lee S, et al. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain. Mol Pain. 2018 Jan-Dec;14:1744806918764979.

Chemical Properties of PLX5622 hemifumarate

Cas No. SDF
Canonical SMILES COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2.O=C(O)/C=C/C(O)=O.[1/2]
Formula C23H21F2N5O3 M.Wt 453.45
Solubility DMSO: 100 mg/mL (220.53 mM); Water: < 0.1 mg/mL (insoluble) 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 PLX5622 hemifumarate

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2053 mL 11.0266 mL 22.0531 mL
5 mM 0.4411 mL 2.2053 mL 4.4106 mL
10 mM 0.2205 mL 1.1027 mL 2.2053 mL
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In vivo Formulation Calculator (Clear solution) of PLX5622 hemifumarate

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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