CP-100356 hydrochloride

Name: CP-100356 hydrochloride
Brand: MedChemExpress
SKU: HY-108347
Rating: 4.5 (2 reviews)

Cat. No.: HY-108347 Purity: 99.19%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC₅₀s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC₅₀=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC₅₀>15 µM).

For research use only. We do not sell to patients.

CP-100356 hydrochloride Chemical Structure

CAS No. : 142715-48-8

Size	Price	Stock	Quantity
5 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE CP-100356 hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 0.5 µM (MDR1), 1.5 µM (BCRP) in MDCKII cells^[1]

In Vitro

CP-100356 (0.1-15 μM; pretreated for 30 min) inhibits acetoxymethyl Calcein (Calcein-AM) uptake and and Digoxin transport in human MDR1-transfected MDCKII cells, with IC₅₀s of 0.50 μM and 1.2 μM, respectively. CP-100356 decreases the BCRP-mediated transport of Prazosin in MDCKII cells, with an IC₅₀ of 1.5 μM^[1].
? CP-100356 (0.064-200 μM; 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC₅₀ of ~66 μM^[1].
? CP-100356 (0-50 μM; 10-30 min) is devoid of inhibition (IC₅₀>50 μM) against the catalytic activity of the individual P450 enzymes including P4503A4 in the competitive inhibition study^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in C_max and AUC at the dose of 24 mg/kg) in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

597.10

Formula

C₃₁H₃₇ClN₄O₆

CAS No.

142715-48-8

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.COC1=CC2=NC(NCCC3=CC=C(OC)C(OC)=C3)=NC(N4CC5=C(C=C(OC)C(OC)=C5)CC4)=C2C=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 11.36 mg/mL (19.03 mM; ultrasonic and warming and heat to 60°C; 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	1.6748 mL	8.3738 mL	16.7476 mL
5 mM	0.3350 mL	1.6748 mL	3.3495 mL
10 mM	0.1675 mL	0.8374 mL	1.6748 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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: ≥ 1.14 mg/mL (1.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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: ≥ 1.14 mg/mL (1.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.14 mg/mL (1.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

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: 99.68%

Select Batch:

Data Sheet (278 KB) SDS (0 KB)

COA (252 KB) LCMS (264 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Kalgutkar AS, et, al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J Pharm Sci. 2009 Dec;98(12):4914-27. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6748 mL	8.3738 mL	16.7476 mL	41.8690 mL
	5 mM	0.3350 mL	1.6748 mL	3.3495 mL	8.3738 mL
	10 mM	0.1675 mL	0.8374 mL	1.6748 mL	4.1869 mL
	15 mM	0.1117 mL	0.5583 mL	1.1165 mL	2.7913 mL