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Encequidar mesylate

Catalog No. T11578L   CAS 849675-87-2
Synonyms: HM30181 mesylate, HM30181A mesylate

Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.

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Encequidar mesylate Chemical Structure
Encequidar mesylate, CAS 849675-87-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 72.00
10 mg In stock $ 98.00
25 mg In stock $ 181.00
50 mg In stock $ 315.00
100 mg In stock $ 495.00
500 mg In stock $ 1,120.00
1 mL * 10 mM (in DMSO) In stock $ 86.00
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Purity: 99.67%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.
In vitro Treatment of 0.1 or 1 nM Encequidar lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM NSC 125973 treatment, respectively [2].
In vivo The plasma concentrations of Encequidar are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h. The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of Encequidar in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction [1].
Synonyms HM30181 mesylate, HM30181A mesylate
Molecular Weight 784.83
Formula C39H40N6O10S
CAS No. 849675-87-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (31.85 mM), sonification is recommended.

TargetMolReferences and Literature

1. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of NSC 125973 as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101. 2. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library NO PAINS Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Drug Repurposing Compound Library Bioactive Compound Library Inhibitor Library Clinical Compound Library

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Keywords

Encequidar mesylate 849675-87-2 Membrane transporter/Ion channel Neuroscience P-gp HM30181A HM 30181 Mesylate HM30181 Mesylate HM 30181 HM30181 mesylate Encequidar Mesylate HM30181 MDR1 ABCB1 HM-30181 Mesylate inhibit CD243 P-glycoprotein Cluster of differentiation 243 HM-30181 Inhibitor HM30181A Mesylate Encequidar Pgp HM30181A mesylate Multidrug resistance protein 1 inhibitor

 

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