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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 205535-74-6
- 分子式: C26H34N2O4
- 分子量:438.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-50879
Elacridar -
HY-10550
Tariquidar -
HY-15255
Zosuquidar -
HY-50671
Zosuquidar trihydrochloride -
HY-13646
Encequidar -
HY-108347
CP-100356 hydrochloride -
HY-50879R
Elacridar (Standard) -
HY-17013
Dofequidar -
HY-13646A
Encequidar mesylate -
HY-10550A
Tariquidar methanesulfonate, hydrate -
HY-13574A
Biricodar -
HY-15134
ONT-093
生物活性
製品説明
Cellular Effect
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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] |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 205535-74-6
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分子量 438.56
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
KR30031 関連分類
HY-123384 関連分類
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