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CP-100356 hydrochloride

Name: CP-100356 hydrochloride
Brand: TargetMol
SKU: T22680
Price: 69 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22680Cas No. 142715-48-8

Alias CP-100356 HCl, CP 100356 hydrochloride

CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters. Additionally, CP-100356 inhibits OATP1B1 and induces stomatal opening in the dark.

CP-100356 hydrochloride

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Purity: 99.19%

Catalog No. T22680Alias CP-100356 HCl, CP 100356 hydrochlorideCas No. 142715-48-8

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$69	-	In Stock

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Purity:99.19%

Appearance:Solid

Color:White

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COA HNMR MS HPLC

Product Introduction

Bioactivity

Description	CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters. Additionally, CP-100356 inhibits OATP1B1 and induces stomatal opening in the dark.
Targets&IC50	MDR1:0.5 µM, BCRP:1.5 µM (in MDCKII cells)
In vitro	In human MDR1-transfected MDCKII cells, CP-100356 hydrochloride inhibited acetoxymethyl calcein (calcein-AM) uptake (IC50 approximately 0.5 +/- 0.07 microM) and digoxin transport (IC50 approximately 1.2 +/- 0.1 microM). Inhibition of prazosin transport (IC50 approximately 1.5 +/- 0.3 microM) in human BCRP-transfected MDCKII cells by CP-100356 hydrochloride confirmed the dual MDR1/BCRP inhibitory properties[1].
In vivo	In vivo inhibitory effects of CP-100356 hydrochloride in rats were examined after coadministration with MDR1 substrate fexofenadine and dual MDR1/BCRP substrate prazosin. Coadministration with increasing doses of CP-100356 hydrochloride resulted in dramatic increases in systemic exposure of fexofenadine (36- and 80-fold increase in C(max) and AUC at a CP-100356 hydrochloride dose of 24 mg/kg). Significant differences in prazosin pharmacokinetics were also discernible in CP-100356 hydrochloride-pretreated rats as reflected from a 2.6-fold increase in AUC.[1].
Synonyms	CP-100356 HCl, CP 100356 hydrochloride

Chemical Properties

Molecular Weight	597.1
Formula	C₃₁H₃₇ClN₄O₆
Cas No.	142715-48-8
Smiles	Cl.COc1ccc(CCNc2nc(N3CCc4cc(OC)c(OC)cc4C3)c3cc(OC)c(OC)cc3n2)cc1OC
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 5 mg/mL (8.37 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.67 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	1.6748 mL	8.3738 mL	16.7476 mL	83.7381 mL
5 mM	0.3350 mL	1.6748 mL	3.3495 mL	16.7476 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc