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

HM30181 mesylate (Synonyms: Encequidar mesylate)

Cat. No.: HY-13646A
Handling Instructions

HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.

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

HM30181 mesylate Chemical Structure

HM30181 mesylate Chemical Structure

CAS No. : 849675-87-2

Size Price Stock
5 mg USD 120 Get quote
10 mg USD 180 Get quote
50 mg USD 504 Get quote
100 mg USD 708 Get quote

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Other In-stock Forms of HM30181 mesylate:

Other Forms of HM30181 mesylate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.

IC50 & Target

P-glycoprotein[1][2].

In Vitro

Compared with control (0 nM HM30181A), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. HM30181A does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without HM30181A. However, treatment of 0.1 or 1 nM HM30181A lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively[2].

In Vivo

The plasma concentrations of HM30181M are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h (p < 0.05). 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 HM30181M 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].

Solvent & Solubility
In Vitro: 

H2O

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
10 mM 0.1274 mL 0.6371 mL 1.2742 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
The cannulised rats are divided into four groups, each comprises of 6 rats. HM30181 M powder or HM30181M- loaded microcapsules are enclosed in hard capsules. One group of rats is dosed orally with paclitaxel solution only, at a drug dose of 20 mg/kg. The rats in the other two groups are administered paclitaxel solution at a drug dose of 20 mg/kg simultaneously with either capsules containing HM30181 M powder or microcapsules (equivalent to 20 mg/kg HM30181 M)[1].

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

References
Molecular Weight

784.83

Formula

C₃₉H₄₀N₆O₁₀S

CAS No.

849675-87-2

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
HM30181 mesylate
Cat. No.:
HY-13646A
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HM30181 mesylate

Cat. No.: HY-13646A