1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
    BCRP
  3. CP-100356 hydrochloride

CP-100356 hydrochloride 

Cat. No.: HY-108347
Handling Instructions

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

CP-100356 hydrochloride Chemical Structure

CAS No. : 142715-48-8

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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)[1].

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].

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 Cmax and AUC at the dose of 24 mg/kg) in rats[1].

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

Molecular Weight

597.10

Formula

C₃₁H₃₇ClN₄O₆

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 44 mg/mL (73.69 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

CP-100356CP100356CP 100356P-glycoproteinBCRPP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Breast cancer resistance proteinABCG2Calcein-AMtransportPrazosinOATP1B1MRP2P450Inhibitorinhibitorinhibit

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Product Name:
CP-100356 hydrochloride
Cat. No.:
HY-108347
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