Home Transmembrane Transporters P-gp inhibitor Encequidar (HM30181) For research use only.

Encequidar (HM30181)

Synonyms: HM30181A

Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).

Encequidar (HM30181) Chemical Structure

Encequidar (HM30181) Chemical Structure

CAS No. 849675-66-7

Purity & Quality Control

Batch: S343101 DMF]50 mg/mL]true]DMSO]Insoluble]false]Water]Insoluble]false Purity: 99.53%
99.53

Encequidar (HM30181) Related Products

Signaling Pathway

P-gp Signaling Pathways

P-gp Signaling Pathway

Biological Activity

Description Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
Targets
P-gp [1]
In vitro
In vitro

HM30181 potently and selectively inhibits Pgp-mediated efflux transport of rhodamine 123 in CCRF-CEM T cells with 13.1±2.3 nM.[1]
Cell Research Cell lines CCRF-CEM T lymphoblast cells
Concentrations 1-100 nM
Incubation Time 5 min
Method

Briefly, cells expressing wild-type Pgp (CCRF-CEM T lymphoblast cell line) were sedimented, the supernatant was removed by aspiration, and the cells were resuspended in Dulbecco’s Modified Eagle’s Medium (DMEM) containing rhodamine 123 at a final concentration of 0.2 μg/ml (0.53 μM). Cells were loaded with fluorochrome for 30 min at 37°C. Tubes were chilled on ice and cells were harvested at 500 × g in an Eppendorf 5403 centrifuge. The cell pellet was washed with ice cold DMEM medium (pH 7.4) and again centrifuged at 500 × g. After resuspension, aliquots of the cell suspension, each containing approximately 1 × 10<sup>6</sup> were transferred to individual fluorescence-activated cell sorter (FACS) tubes and again centrifuged. Supernatants were removed, and the pellets were resuspended individually in prewarmed DMEM medium (pH 7.4) containing either no inhibitor or HM30181 mesylate or elacridar hydrochloride or tariquidar dimesylate at various concentrations in DMSO ranging from 1 to 100 nM. Right after resuspending cells each individual tube was placed in a temperature controlled unit and cell associated fluorescence was monitored over a period of 5 min with a FACS system.
In Vivo
In vivo

PET scans with the Pgp substrate (R)-[11C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) fails to show significant increases in (R)-[11C]verapamil brain uptake compared with vehicle treated animals.[1]
Animal Research Animal Models Female Mdr1a/b(−/−), Bcrp1(−/−) and Mdr1a/b(−/−)Bcrp1(−/−) mice with a FVB genetic background
Dosages 10 or 21 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03892018 Terminated
Solid Tumor Adult
Athenex Inc.
 August 5 2019 Phase 1
NCT02963168 Unknown status
Solid Tumor
Athenex Inc.
 April 20 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 688.73 Formula

C38H36N6O7
CAS No. 849675-66-7 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMF : 50 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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