1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp inhibitor 1

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

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

P-gp inhibitor 1 Chemical Structure

P-gp inhibitor 1 Chemical Structure

CAS No. : 2050747-49-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 182 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

IC50 & Target

P-glycoprotein[1]

In Vitro

P-gp inhibitor 1 (12k) possesses high potency (EC50=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes)[1].

P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour)[1].

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

Western Blot Analysis[1]

Cell Line: K562/A02 cell
Concentration: 0.1, 0.5, or 2.0 μM
Incubation Time: 72 hours
Result: MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux[1].
Molecular Weight

517.62

Formula

C32H31N5O2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

COC(C(OC)=C1)=CC2=C1CCN(C2)CCC3=CC=C(NC4=NC(C5=CC=NC=C5)=NC6=CC=CC=C46)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (32.21 mM; ultrasonic and warming and heat to 70°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 1.9319 mL 9.6596 mL 19.3192 mL
5 mM 0.3864 mL 1.9319 mL 3.8638 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9319 mL 9.6596 mL 19.3192 mL 48.2980 mL
5 mM 0.3864 mL 1.9319 mL 3.8638 mL 9.6596 mL
10 mM 0.1932 mL 0.9660 mL 1.9319 mL 4.8298 mL
15 mM 0.1288 mL 0.6440 mL 1.2879 mL 3.2199 mL
20 mM 0.0966 mL 0.4830 mL 0.9660 mL 2.4149 mL
25 mM 0.0773 mL 0.3864 mL 0.7728 mL 1.9319 mL
30 mM 0.0644 mL 0.3220 mL 0.6440 mL 1.6099 mL
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P-gp inhibitor 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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