CP-100356 hydrochloride
Based on 9 publication(s) in Google Scholar
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.
- Purity: 99.12%
- CAS No.: 142715-48-8
- Formula: C31H37ClN4O6
- Molecular Weight:597.10
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Orally Active Compound Library
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Publications Citing Use of MedChemExpress (MCE) CP-100356 hydrochloride
More- Commun Med (Lond). 2025 Apr 26;5(1):140. [Abstract]
- J Med Chem. 2024 Jun 13;67(11):8757-8790. [Abstract]
- Molecules. 2025 Jan 17;30(2):387. [Abstract]
- Antimicrob Agents Chemother. 2025 Apr 2;69(4):e0155624. [Abstract]
- SLAS Discov. 2024 Jul;29(5):100160. [Abstract]
- bioRxiv. 2025 Nov 3.
- Res Sq. 2024 Nov 25.
- Preprints. 2024 Jan 3.
- Preprints. 2022, 2022050381.
Biological Activity
IC50: 0.5 µM (MDR1), 1.5 µM (BCRP) in MDCKII cells[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 142715-48-8
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Appearance Solid
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Molecular Weight 597.10
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Formula C31H37ClN4O6
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Commun Med (Lond)
Targeted protein degraders of SARS-CoV-2 Mpro are more active than enzymatic inhibition alone with activity against nirmatrelvir resistant virus. [Abstract]2025 Apr 26;5(1):140. PMID: 40287552 -
J Med Chem
Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs. [Abstract]2024 Jun 13;67(11):8757-8790. PMID: 38753594 -
Molecules
Antiviral Activity and Underlying Mechanism of Moslae herba Aqueous Extract for Treating SARS-CoV-2. [Abstract]2025 Jan 17;30(2):387. PMID: 39860255 -
Antimicrob Agents Chemother
Potent antiviral activity of simnotrelvir against key epidemic SARS-CoV-2 variants with a high resistance barrier. [Abstract]2025 Apr 2;69(4):e0155624. PMID: 40062859 -
SLAS Discov
2024 Jul;29(5):100160. PMID: 38761981 -
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Solvent & Solubility
DMSO : 100 mg/mL (167.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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
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.
| 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 | |
| 20 mM | 0.0837 mL | 0.4187 mL | 0.8374 mL | 2.0935 mL | |
| 25 mM | 0.0670 mL | 0.3350 mL | 0.6699 mL | 1.6748 mL | |
| 30 mM | 0.0558 mL | 0.2791 mL | 0.5583 mL | 1.3956 mL | |
| 40 mM | 0.0419 mL | 0.2093 mL | 0.4187 mL | 1.0467 mL | |
| 50 mM | 0.0335 mL | 0.1675 mL | 0.3350 mL | 0.8374 mL | |
| 60 mM | 0.0279 mL | 0.1396 mL | 0.2791 mL | 0.6978 mL | |
| 80 mM | 0.0209 mL | 0.1047 mL | 0.2093 mL | 0.5234 mL | |
| 100 mM | 0.0167 mL | 0.0837 mL | 0.1675 mL | 0.4187 mL |
CP-100356 hydrochloride Related Classifications
HY-108347 Related Classifications
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