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GPV0057

GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome[1][2].

Product Specifications

CAS Number

86383-89-3

UNSPSC

12352005

Target

P-glycoprotein; Potassium Channel

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Cancer; Cardiovascular Disease

Purity

99.20

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(CCC1=CC=CC=C1)C2=C(OCC(CN3CCOCC3)O)C=CC=C2

Molecular Formula

C22H27NO4

Molecular Weight

369.45

References & Citations

[1]Cseke A, et al. Propafenone analogue with additional H-bond acceptor group shows increased inhibitory activity on P-glycoprotein. Arch Pharm (Weinheim) . 2020 Mar;353 (3) :e1900269.|[2]Li E, et al. Development of new Kir2.1 channel openers from propafenone analogues. Br J Pharmacol. 2025 Feb;182 (3) :633-650.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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