849675-66-7
849675-66-7 structure
- Name: HM30181
- Chemical Name: HM30181
- CAS Number: 849675-66-7
- Molecular Formula: C38H36N6O7
- Molecular Weight: 688.728
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
- Create Date: 2018-06-04 09:59:56
- Modify Date: 2024-01-14 19:00:38
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HM30181 is a potent and selective inhibitor of P-glycoprotein.
| Name | HM30181 |
|---|---|
| Synonyms |
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
K4I4I996O4 HM-30181 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- MFCD25976625 4-oxo-4H-chromene-2-carboxylic acid (2-(2-(4-(2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl)-phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)amide HM30181A |
| Description | HM30181 is a potent and selective inhibitor of P-glycoprotein. |
|---|---|
| Related Catalog | |
| In Vitro | HM30181 is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, HM30181: 13.1±2.3 nM) [1]. HM30181 shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor[2]. |
| In Vivo | PET scans with the Pgp substrate (R)-[11C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]verapamil brain uptake compared with vehicle treated animals[1]. 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. HM30181 increases the oral bioavailability of co-administered paclitaxel by more than 12 times in rats[2]. |
| Animal Admin | Mice: HM30181 mesylate is dissolved in 5% aqueous glucose solution, containing 20 μL 0.01 M aq. HCl and injected at a volume of 4 mL/kg. Female FVB wild-type mice, aged 8-12 weeks weighing 24±4 g undergo (R)-[11C]verapamil PET scans without and with i.v. pretreatment with cold HM30181. Animals are assigned to 5 groups (n=4 per group). One group is pretreated with HM30181 vehicle solution (5% aq. glucose solution containing 20 μL 0.01 M aq. HCl) at 60 min before start of the PET scan. The other groups are pretreated with either 10 mg/kg HM30181 at 10, 60 or 120 min before PET or with 21 mg/kg HM30181 at 10 min before PET[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C38H36N6O7 |
| Molecular Weight | 688.728 |
| Exact Mass | 688.264526 |
| LogP | 7.14 |
| Index of Refraction | 1.663 |