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Encequidar

Catalog No. T8426   CAS 849675-66-7
Synonyms: HM30181, HM30181A

Encequidar (HM30181A) is a potent and selective P-glycoprotein inhibitor.

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Encequidar Chemical Structure
Encequidar, CAS 849675-66-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 97.00
10 mg In stock $ 147.00
25 mg In stock $ 259.00
50 mg In stock $ 401.00
100 mg In stock $ 587.00
1 mL * 10 mM (in DMSO) In stock $ 136.00
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Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Encequidar (HM30181A) is a potent and selective P-glycoprotein inhibitor.
In vivo HM30181 to inhibit Pgp at the murine BBB.?HM30181 was shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC(50), tariquidar: 8.2 2.0 nM, HM30181: 13.1 2.3 nM).?PET scans with the Pgp substrate (R)-[(11)C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failed to show significant increases in (R)-[(11)C]verapamil brain uptake compared with vehicle treated animals.?PET scans with [(11)C]HM30181 showed low and not significantly different brain uptake of [(11)C]HM30181 in wild-type, Mdr1a/b((-/-)) and Bcrp1((-/-)) mice and significantly, i.e. 4.7-fold (P<0.01), higher brain uptake, relative to wild-type animals, in Mdr1a/b((-/-))Bcrp1((-/-)) mice[1].
Synonyms HM30181, HM30181A
Molecular Weight 688.73
Formula C38H36N6O7
CAS No. 849675-66-7

Storage

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

Solubility Information

DMSO: 6.9 mg/mL (10.02 mM), Sonification is recommended

TargetMolReferences and Literature

1. Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27. 2. Jin Cheul Kim , Kyeong Soo Kim , Dong Shik Kim,et al.Effect of HM30181 Mesylate Salt-Loaded Microcapsules on the Oral Absorption of Paclitaxel as a Novel P-glycoprotein Inhibitor.Int J Pharm. 2016 Jun 15;506(1-2):93-101.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Ion Channel Inhibitor Library ReFRAME Related Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

Encequidar 849675-66-7 Membrane transporter/Ion channel Neuroscience P-gp MDR1 Cluster of differentiation 243 inhibit P-glycoprotein HM30181 Multidrug resistance protein 1 Inhibitor CD243 HM-30181 Pgp ABCB1 HM 30181 HM30181A inhibitor

 

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