| 產(chǎn)品描述： | Encequidar (HM30181, HM30181A) 是一種有效的、選擇性的三磷酸腺苷結(jié)合盒轉(zhuǎn)運體 P-glycoprotein (P-gp) 的抑制劑 |
| 靶點： |
P-gp |
| 體外研究： |
HM30181 potently and selectively inhibits Pgp-mediated efflux transport of rhodamine 123 in CCRF-CEM T cells with 13.1±2.3 nM |
| 體內(nèi)研究： |
PET scans with the Pgp substrate (R)-[11C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) fails to show significant increases in (R)-[11C]verapamil brain uptake compared with vehicle treated animals. |
| 細胞實驗： |
Cell lines: CCRF-CEM T lymphoblast cells Concentrations: 1-100 nM Incubation Time: 5 min Method: Briefly, cells expressing wild-type Pgp (CCRF-CEM T lymphoblast cell line) were sedimented, the supernatant was removed by aspiration, and the cells were resuspended in Dulbecco’s Modified Eagle’s Medium (DMEM) containing rhodamine 123 at a final concentration of 0.2 μg/ml (0.53 μM). Cells were loaded with fluorochrome for 30 min at 37°C. Tubes were chilled on ice and cells were harvested at 500 × g in an Eppendorf 5403 centrifuge. The cell pellet was washed with ice cold DMEM medium (pH 7.4) and again centrifuged at 500 × g. After resuspension, aliquots of the cell suspension, each containing approximately 1 × 106 were transferred to individual fluorescence-activated cell sorter (FACS) tubes and again centrifuged. Supernatants were removed, and the pellets were resuspended individually in prewarmed DMEM medium (pH 7.4) containing either no inhibitor or HM30181 mesylate or elacridar hydrochloride or |
| 動物實驗： |
Animal Models: Female Mdr1a/b(?/?), Bcrp1(?/?) and Mdr1a/b(?/?)Bcrp1(?/?) mice with a FVB genetic background Dosages: 10 or 21 mg/kg Administration: i.v. |
| 參考文獻： |
1. Florian Bauer, 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. |
| 溶解性： |
soluble in DMF |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.452 ml |
7.26 ml |
14.52 ml |
| 5 mM |
0.29 ml |
1.452 ml |
2.904 ml |
| 10 mM |
0.145 ml |
0.726 ml |
1.452 ml |
| 50 mM |
0.029 ml |
0.145 ml |
0.29 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京