Home Transmembrane Transporters P-gp inhibitor Encequidar (HM30181)

research use only

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

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

Solubility

In vitro
Batch:

DMF : 50 mg/mL

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

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
P-gp [1]
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]
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map