| Identification | Back Directory | [Name]
HM30181 (Mesylate) | [CAS]
849675-87-2 | [Synonyms]
HM30181A mesylate
HM30181 (Mesylate)
Encequidar mesylate
PEKXWELLWNPUOK-UHFFFAOYSA-N
Encequidar mesylate (HM-30181
HM30181 mesylate (Encequidar mesylate)
HM30181 mesylate (Synonyms: Encequidar mesylate)
HM30181A,HM 30181,Encequidar mesylate,HM30181,MDR1,ABCB1,P-gp,inhibit,CD243,P-glycoprotein,Cluster of differentiation 243,HM-30181,Inhibitor,Encequidar,Pgp,Multidrug resistance protein 1 | [Molecular Formula]
C39H40N6O10S | [MOL File]
849675-87-2.mol | [Molecular Weight]
784.84 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:25.0(Max Conc. mg/mL);31.85(Max Conc. mM) | [form ]
Solid | [color ]
Light yellow to yellow | [InChIKey]
PEKXWELLWNPUOK-UHFFFAOYSA-N | [SMILES]
S(O)(=O)(=O)C.N(C1C=C(OC)C(OC)=CC=1C1N=NN(C2C=CC(CCN3CCC4=CC(OC)=C(OC)C=C4C3)=CC=2)N=1)C(C1=CC(=O)C2=CC=CC=C2O1)=O |
| Hazard Information | Back Directory | [Uses]
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor. | [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]. | [References]
[1] Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of NSC 125973 as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101. DOI:10.1016/j.ijpharm.2016.04.034
[2] Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12. PMID:18813783 |
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