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Valspodar

Name: Valspodar
Brand: TargetMol
SKU: T17216
Price: 212 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: PSC 833) Copy Product Info

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Synonyms: PSC 833

Catalog No. T17216 Copy Product Info

Purity: 99.26%

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Valspodar (PSC 833) is a small-molecule inhibitor and a P-glycoprotein (P-gp) inhibitor with high selectivity and chemosensitizing properties. This compound can effectively reverse P-gp-mediated multidrug resistance (MDR) and is used in experimental research on drug-resistant tumors such as advanced epithelial ovarian cancer.

Cas No. 121584-18-7

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Pack Size	Price	USA Stock	Global Stock
1 mg	$212	In Stock	In Stock
5 mg	$639	In Stock	In Stock
10 mg	$987	-	In Stock
25 mg	$1,980	-	In Stock
50 mg	$3,290	-	In Stock
1 mL x 10 mM (in DMSO)	$1,370	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:99.26%

Appearance:Solid

Color:White

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COA HNMR MS

Product Introduction

Bioactivity

Description	Valspodar (PSC 833) is a small-molecule inhibitor and a P-glycoprotein (P-gp) inhibitor with high selectivity and chemosensitizing properties. This compound can effectively reverse P-gp-mediated multidrug resistance (MDR) and is used in experimental research on drug-resistant tumors such as advanced epithelial ovarian cancer.
Targets & IC50	SW620 cells:0.1 μM, L929 cells:> 100 μM, MDR cells:0.4 μM
In vitro	Methods: A Caco-2 cell monolayer model was used. Bidirectional transport experiments were performed with 4 μM Valspodar co-incubated with ticagrelor for 3 hours. Results: Valspodar significantly reduced the basolateral-to-apical apparent permeability coefficient of ticagrelor (from 1.60×10⁻⁵ to 1.13×10⁻⁵ cm/s), with the efflux ratio decreasing from 2.71 to 1.59 and an inhibition rate of approximately 70%, confirming that Valspodar can effectively inhibit P-gp-mediated ticagrelor efflux. [1] Methods: P-glycoprotein (P-gp)-overexpressing human breast cancer MCF-7 TX400 cells were used. Valspodar at 3 μg/mL was co-incubated with photosensitizers for 1 hour, and detection was performed by extraction method and flow cytometry. Results: Valspodar increased intracellular accumulation of BPD and rose bengal, suggesting that both are P-gp substrates; Results for ropurpurin were inconsistent, while other photosensitizers such as temoporfin showed no significant effect. [2]
In vivo	Methods: An NMRI nu/nu mouse model was used. Valspodar was administered orally by gavage at a dose of 50 mg/kg (dissolved in DMSO/PEG/water) as a single dose 4 hours before paclitaxel injection. Results: Valspodar increased brain concentrations of paclitaxel by 6–8 fold, but also significantly increased paclitaxel levels in liver, kidney, and plasma, with a relatively low brain/plasma ratio.[3] Methods:Sprague Dawley rats were used. Valspodar was administered by constant-rate infusion via femoral vein at doses of 0.09–8 mg/hr/kg for 4.5 hours, dissolved in Cremophor EL:ethanol:normal saline. Results: At doses ≥0.9 mg/hr/kg, the brain/plasma ratio of P-gp substrates such as loperamide and quinidine no longer increased with dose, indicating that this dose can completely inhibit P-gp-mediated efflux at the blood-brain barrier.[4]
Synonyms	PSC 833

Chemical Properties

Molecular Weight	1214.62
Formula	C₆₃H₁₁₁N₁₁O₁₂
Cas No.	121584-18-7
Smiles	C\C=C\C[C@@H](C)C(=O)[C@@H]1N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@@H](NC1=O)C(C)C)C(C)C
Relative Density.	1.015 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (74.1 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 3.3 mg/mL (2.72 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8233 mL	4.1165 mL	8.2330 mL	41.1651 mL
5 mM	0.1647 mL	0.8233 mL	1.6466 mL	8.2330 mL
10 mM	0.0823 mL	0.4117 mL	0.8233 mL	4.1165 mL
20 mM	0.0412 mL	0.2058 mL	0.4117 mL	2.0583 mL
50 mM	0.0165 mL	0.0823 mL	0.1647 mL	0.8233 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.