1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Encequidar

Encequidar (Synonyms: HM30181; HM30181A)

Cat. No.: HY-13646 Purity: 98.12%
Handling Instructions

Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

For research use only. We do not sell to patients.

Encequidar Chemical Structure

Encequidar Chemical Structure

CAS No. : 849675-66-7

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Based on 1 publication(s) in Google Scholar

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Description

Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

In Vitro

Encequidar (HM30181; HM30181A) is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar (HM30181): 13.1±2.3 nM) [1].
Encequidar (HM30181) shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor[2].

In Vivo

PET scans with the Pgp substrate (R)-[11C]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]NSC 657799 brain uptake compared with vehicle treated animals[1].
Encequidar (HM30181) inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. Encequidar (HM30181) increases the oral bioavailability of co-administered NSC 125973 by more than 12 times in rats[2].

Clinical Trial
Molecular Weight

688.73

Formula

C₃₈H₃₆N₆O₇

CAS No.

849675-66-7

SMILES

O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.9 mg/mL (10.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4519 mL 7.2597 mL 14.5195 mL
5 mM 0.2904 mL 1.4519 mL 2.9039 mL
10 mM 0.1452 mL 0.7260 mL 1.4519 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Encequidar (HM30181) mesylate is dissolved in 5% aqueous glucose solution, containing 20 μL 0.01 M aq. HCl and injected at a volume of 4 mL/kg. Female FVB wild-type mice, aged 8-12 weeks weighing 24±4 g undergo (R)-[11C]NSC 657799 PET scans without and with i.v. pretreatment with cold Encequidar (HM30181). Animals are assigned to 5 groups (n=4 per group). One group is pretreated with HM30181 vehicle solution (5% aq. glucose solution containing 20 μL 0.01 M aq. HCl) at 60 min before start of the PET scan. The other groups are pretreated with either 10 mg/kg Encequidar (HM30181) at 10, 60 or 120 min before PET or with 21 mg/kg HM30181 at 10 min before PET[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

EncequidarHM30181HM30181AHM 30181HM-30181P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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