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.
For research use only. We do not sell to patients.
- CAS No.: 205535-74-6
- Formula: C26H34N2O4
- Molecular Weight:438.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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 No. 205535-74-6
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Molecular Weight 438.56
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KR30031 Related Classifications
HY-123384 Related Classifications
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