KR30031
KR30031, a Verapamil (HY-14275) analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting P-gp with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer.
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- CAS. Nr.: 205535-74-6
- Formel: C26H34N2O4
- Molecular Weight:438.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-50879
Elacridar
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HY-10550
Tariquidar
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HY-15255
Zosuquidar
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HY-50671
Zosuquidar trihydrochloride
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HY-13646
Encequidar
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HY-108347
CP-100356 hydrochloride
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HY-50879R
Elacridar (Standard)
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HY-17013
Dofequidar
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HY-13646A
Encequidar mesylate
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HY-10550A
Tariquidar methanesulfonate, hydrate
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HY-13574A
Biricodar
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HY-15134
ONT-093
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| MES-SA/Dx5 | IC50 |
7.63 μM
Compound: KR30031 (racemic)
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TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
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[PMID: 12569305] |
KR30031 (0.01-100 μM) produces concentration-dependent relaxation of aorta precontracted with 60 mM KCl, with an EC50 of 9.14 μM[1].
KR30031 (0.0001-100 mM) induces a concentration-dependent decrease in left ventricular pressure (LVP) of isolated hearts, with an EC50 of 11.6 mM; it also causes a concentration-dependent decrease in heart rate (HR) of isolated hearts[1].
KR30031 (0.3-10.0 μM, 72 h) enhances Paclitaxel (HY-B0015)-induced cytotoxicity to HCT15/CL02 and MES-SA/DX5 cells with high P-glycoprotein expression, with IC50 values of 3.20 μM and 7.63 μM, respectively[1].
KR30031 (0.3-100 μM, 72 h) shows intrinsic cytotoxicity to HCT15/CL02 and MES-SA/DX5 cells only at 100 μM[1].
KR30031 (25 μM) increases apical-to-basolateral transport of Paclitaxel in Caco-2 cell monolayer, with potency equal to Verapamil (HY-14275)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 205535-74-6
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Molecular Weight 438.56
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Formel C26H34N2O4
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SMILES
N#CC1(CCC2=C1C=CC(OC)=C2OC)CCCN(C)CCC3=CC=C(C(OC)=C3)OC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Lee BH, et al. Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. Anticancer Drugs. 2003 Feb;14(2):175-81. [Content Brief]
[2]. Woo JS, et al. Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031. Pharm Res. 2003 Jan;20(1):24-30. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KR30031 Related Classifications
HY-123384 Related Classifications
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