86383-89-3
Chemical Structure
GPV0057
- CAS No.: 86383-89-3
- Formula:C22H27NO4
- Molecular Weight:369.45
InChIKey: POGUJMYEESQTCM-UHFFFAOYSA-N
SMILES: O=C(CCC1=CC=CC=C1)C2=C(OCC(CN3CCOCC3)O)C=CC=C2
Biological Activity: 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].
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GPV0057 | 99.20% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Li E, et al. Development of new Kir2.1 channel openers from propafenone analogues. Br J Pharmacol. 2025 Feb;182(3):633-650. [Content Brief]
Keywords
