849675-87-2
849675-87-2 structure
- Name: HM30181 mesylate (Encequidar mesylate)
- Chemical Name: HM30181 mesylate
- CAS Number: 849675-87-2
- Molecular Formula: C39H40N6O10S
- Molecular Weight: 784.834
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
- Create Date: 2019-01-20 19:23:21
- Modify Date: 2024-01-12 20:02:56
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HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.
| Name | HM30181 mesylate |
|---|---|
| Synonyms |
4H-1-Benzopyran-2-carboxamide, N-[2-[2-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-2H-tetrazol-5-yl]-4,5-dimethoxyphenyl]-4-oxo-, methanesulfonate (1:1)
Encequidar Mesylate N-[2-(2-{4-[2-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl]-4-oxo-4H-chromene-2-carboxamide methanesulfonate (1:1) HM-30181 MESYLATE |
| Description | HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor. |
|---|---|
| Related Catalog | |
| 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C39H40N6O10S |
|---|---|
| Molecular Weight | 784.834 |
| Exact Mass | 784.252686 |