N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride

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N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Suppliers list
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N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride manufacturers
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Basic information
Product Name:N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride
Synonyms:N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride;XR 9051 HCl;XR9051 (hydrochloride);3-[(Z)-[(5Z)-5-benzylidene-4-methyl-3,6-dioxopiperazin-2-ylidene]methyl]-N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]benzamide:hydrochloride;XR9051 Hydrochloride,XR-9051 Hydrochloride
CAS:180422-22-4
MF:C39H39ClN4O5
MW:679.21
EINECS:
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Mol File:180422-22-4.mol
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Structure
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Chemical Properties
storage temp. Store at -20°C
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MSDS Information
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Usage And Synthesis
UsesXR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR)[1].
in vivo

XR9051 (20-40 mg/kg, ip) shows significant modulatory activity in mice bearing MDR human ovarian (2780AD and CH1/DOXr) and SCLC (H69/LX) xenografts[2].

Animal Model:Female Balb/c mice (20-25 g)[2].
Dosage:I.V.
Administration:20 mg/kg at various times (5 min to 24 h).
Result:The area under the concentration time curves (AUC) from time 0-∞ for plasma was 11.9 μg. h mL-1. The ratio between AUC for tissue:plasma for liver, heart and brain were 79.6, 16.9 and 0.3 respectively.
Animal Model:MDR 2780AD ovarian carcinoma xenografts[2].
Dosage:I.P.
Administration:20, 30, 40 mg/kg daily with Epirubicin i.v. (10 mg/kg).
Result:Significantly reduced growth rate of MDR 2780AD ovarian carcinoma xenografts compared with either drug alone.
References[1] I L Dale , et al. Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer. 1998 Oct;78(7):885-92. DOI:10.1038/bjc.1998.597
[2] P Mistry, et al. In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance. Br J Cancer. 1999 Apr;79(11-12):1672-8. DOI:10.1038/sj.bjc.6690267
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride Preparation Products And Raw materials
Tag:N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamidehydrochloride(180422-22-4) Related Product Information
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