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

Encequidar mesylate  (Synonyms: HM30181 mesylate; HM30181A mesylate)

Cat. No.: HY-13646A Purity: 99.84%
COA Handling Instructions

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Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.

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

Encequidar mesylate Chemical Structure

Encequidar mesylate Chemical Structure

CAS No. : 849675-87-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 86 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Encequidar mesylate:

Encequidar mesylate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.

IC50 & Target

P-glycoprotein[1][2].
In Vitro

Treatment of 0.1 or 1 nM Encequidar (HM30181) lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM NSC 125973 treatment, respectively[2].

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

Encequidar mesylate Related Antibodies
In Vivo

The plasma concentrations of Encequidar (HM30181) are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h. The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of Encequidar (HM30181) in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

784.83

Formula

C39H40N6O10S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (31.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2742 mL 6.3708 mL 12.7416 mL
5 mM 0.2548 mL 1.2742 mL 2.5483 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

COA (254 KB) HNMR (325 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Rats[1]
The cannulised rats are divided into four groups, each comprises of 6 rats. Encequidar (HM30181) powder or Encequidar (HM30181)- loaded microcapsules are enclosed in hard capsules. One group of rats is dosed orally with NSC 125973 solution only, at a drug dose of 20 mg/kg. The rats in the other two groups are administered NSC 125973 solution at a drug dose of 20 mg/kg simultaneously with either capsules containing Encequidar (HM30181) powder or microcapsules (equivalent to 20 mg/kg Encequidar (HM30181))[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2742 mL 6.3708 mL 12.7416 mL 31.8540 mL
5 mM 0.2548 mL 1.2742 mL 2.5483 mL 6.3708 mL
10 mM 0.1274 mL 0.6371 mL 1.2742 mL 3.1854 mL
15 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1236 mL
20 mM 0.0637 mL 0.3185 mL 0.6371 mL 1.5927 mL
25 mM 0.0510 mL 0.2548 mL 0.5097 mL 1.2742 mL
30 mM 0.0425 mL 0.2124 mL 0.4247 mL 1.0618 mL
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Encequidar mesylate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Encequidar849675-87-2HM30181HM30181AHM 30181HM-30181P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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