Home Transmembrane Transporters P-gp inhibitor Encequidar (HM30181)

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Encequidar (HM30181) P-gp inhibitor

Cat.No.S3431

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

Chemical Structure

Molecular Weight: 688.73

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Quality Control

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

Solubility

In vitro
Batch:

DMF : 50 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 688.73 Formula

C38H36N6O7

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

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC50/Ki
P-gp
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-06)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01042379 RECRUITING
Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
QuantumLeap Healthcare Collaborative
 2010-03-01 PHASE2
NCT06835400 NOT_YET_RECRUITING
Metastatic Breast Cancer
Health Hope Pharma
 2025-09 PHASE3
NCT07580833 NOT_YET_RECRUITING
Metastatic Breast Cancer
Health Hope Pharma
 2026-05 PHASE1
NCT04180384 COMPLETED
Solid Tumor
Athenex, Inc.
 2015-09-23 PHASE2
NCT03892018 Terminated
Solid Tumor Adult
Athenex Inc.
 2019-08-05 Phase 1
NCT04035473 COMPLETED
Solid Tumor
Athenex, Inc.
 2015-08-01 PHASE1

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