Encequidar (HM30181)
(Synonyms: HM30181; HM30181A) 目录号 : GC31340
An inhibitor of P-glycoprotein
Cas No.:849675-66-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
HM30181 is an inhibitor of P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1; IC50 = 0.63 nM).1 It is selective for P-gp over breast cancer resistance protein (BCRP; IC50 = 3,700 nM), as well as multidrug resistance-associated protein 1 (MRP1), MRP2, and MRP3 at 100 ?M. It inhibits transepithelial basal-to-apical transport of paclitaxel in MDCK monolayers overexpressing P-gp (IC50 = 35.4 nM). HM30181 inhibits tumor growth and induces tumor regression in an HT-29 mouse xenograft model when administered at doses of 10 and 20 mg/kg, respectively, in combination with paclitaxel .
1.Kwak, J.-O., Lee, S.H., Lee, G.S., et al.Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxelEur. J. Pharmacol.627(1-3)92-98(2009)
|
Animal experiment: |
Mice[1]Encequidar (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 Encequidar (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 Encequidar (HM30181) at 10, 60 or 120 min before PET or with 21 mg/kg HM30181 at 10 min before PET[1]. |
|
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. |
|
| Cas No. | 849675-66-7 | SDF | |
| 别名 | HM30181; HM30181A | ||
| Canonical SMILES | O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4 | ||
| 分子式 | C38H36N6O7 | 分子量 | 688.73 |
| 溶解度 | 2.4mg/mL in DMSO (Need ultrasonic); 50mg/mL in DMF (Need ultrasonic). | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4519 mL | 7.2597 mL | 14.5195 mL |
| 5 mM | 0.2904 mL | 1.4519 mL | 2.9039 mL |
| 10 mM | 0.1452 mL | 0.726 mL | 1.4519 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet