HM 30181A manufacturers
- Encequidar
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- $41.00 / 1mg
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2024-11-19
- CAS:849675-66-7
- Min. Order:
- Purity: 99.93%
- Supply Ability: 10g
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| | HM 30181A Basic information |
| Product Name: | HM 30181A | | Synonyms: | HM 30181A;HM30181;HM30181A;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-;HM30181(Encequidar);Encequidar (HM-30181;HM30181;MDR1,P-gp,Cluster of differentiation 243,inhibit,HM 30181,Encequidar,P-glycoprotein,Multidrug resistance protein 1,Inhibitor,CD243,Pgp,ABCB1,HM-30181;Encequidar, 10 mM in DMSO | | CAS: | 849675-66-7 | | MF: | C38H36N6O7 | | MW: | 688.73 | | EINECS: | | | Product Categories: | | | Mol File: | 849675-66-7.mol |  |
| | HM 30181A Chemical Properties |
| density | 1.35±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF:30.0(Max Conc. mg/mL);43.56(Max Conc. mM) | | form | A crystalline solid | | pka | 7.95±0.70(Predicted) | | color | Light yellow to yellow |
| | HM 30181A Usage And Synthesis |
| Uses | Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. | | in vivo | PET scans with the Pgp substrate (R)-[11C]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]NSC 657799 brain uptake compared with vehicle treated animals[1]. Encequidar (HM30181) inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. Encequidar (HM30181) increases the oral bioavailability of co-administered NSC 125973 by more than 12 times in rats[2]. | | References | [1] Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27. DOI:10.1016/j.ejphar.2012.09.013
[2] Kim TE, et al. Effects of HM30181, a P-glycoprotein inhibitor, on the pharmacokinetics and pharmacodynamics of loperamide in healthy volunteers. Br J Clin Pharmacol. 2014 Sep;78(3):556-64. DOI:10.1111/bcp.12368 |
| | HM 30181A Preparation Products And Raw materials |
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