CP-100356
Based on 9 publication(s) in Google Scholar
CP-100356 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 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM).
For research use only. We do not sell to patients.
- CAS No.: 142716-85-6
- Formula: C31H36N4O6
- Molecular Weight:560.64
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) CP-100356
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.
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
-
Cell Proliferation/Viability Assay
Biological Activity
Description
Chemical Information
-
CAS No. 142716-85-6
-
Molecular Weight 560.64
-
Formula C31H36N4O6
-
SMILES
COC1=CC2=NC(NCCC3=CC=C(C(OC)=C3)OC)=NC(N4CC5=C(CC4)C=C(C(OC)=C5)OC)=C2C=C1OC
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
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
CP-100356 purchased from MedChemExpress. Usage Cited in: SLAS Discov. 2024 Jul;29(5):100160. [Abstract]
CP-100356 hydrochloride (EI; 1 μM) showed CPE inhibition with an IC50 of 0.047 μM when combined with PF-07321332 in Vero E6 cells with enhanced ACE-2 expression infected with the WA1/2020 isolate of SARS-CoV-2.
CP-100356 purchased from MedChemExpress. Usage Cited in: SLAS Discov. 2024 Jul;29(5):100160. [Abstract]
CP-100356 hydrochloride (0-100 μM) showed cytotoxic activity with a CC50 value of 6.81 μM for Vero E6 cells.
-
CP-100356 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 3.
CP-100356 hydrochloride (0.5-1.5 μM; 72 h) increased FT235 antiviral activity against the ancestral B.1 86 strain.
CP-100356 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 3.
CP-100356 hydrochloride (0.5, 1, 1.5 μM; 72 h) increased FT235 antiviral activity against SARS-CoV-2 141 B.1 variant.
CP-100356 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 3.
CP-100356 hydrochloride (0.5 μM; 72 h) showed no measurable activity against the Omicron BA.5 variant.
-
-
-
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)