AZ 10606120 dihydrochloride
目录号 : GC17375
A P2X7 receptor antagonist
Cas No.:607378-18-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KD: 1.4 nM and 1.9 nM for human and rat P2X7 receptors, respectivley
The P2X7 receptor has intriguing biophysical properties, activates a diverse range of cellular events and mediates a wide range of functional effects. The P2X7 receptor is an ATP-gated ion channel known for its cytotoxic activity. However, recent evidence suggests a role for P2X7 in cell proliferation. AZ 10606120 is a P2X7 receptor antagonist.
In vitro: Binding of [3H]-AZ 10606120 was higher in membranes prepared from cells expressing P2X7 receptors than from control cells and was inhibited by ATP suggesting labelled sites represented human P2X7 receptors. Binding was reversible, saturable and modulated by P2X7 receptor ligands. The positive cooperativity observed suggests that binding of AZ 10606120 to one subunit in the P2X7 receptor complex enhances subsequent binding to other P2X7 subunits in the same complex. The negative cooperative effects of ATP suggest that ATP and AZ 10606120 bind at separate, interacting, sites on the P2X7 receptor [1].
In vivo: Intratumor injection of AZ10606120 caused a strong inhibition of tumor growth in B16-inoculated C57Bl/6 mice and caused in parallel a large reduction in VEGF staining and vessel formation [2].
Clinical trial: Up to now, AZ 10606120 is still in the preclinical development stage.
Reference:
[1] AD Michel, LJ Chambers, WC Clay, JP Condreay, DS Walter and IP Chessell. Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding. British Journal of Pharmacology (2007) 151, 84–95
[2] Elena Adinolfi, Lizzia Raffaghello, Anna Lisa Giuliani, Luigi Cavazzini, Marina Capece, Paola Chiozzi, Giovanna Bianchi, Guido Kroemer, Vito Pistoia, and Francesco Di Virgilio. Expression of P2X7 Receptor Increases In Vivo Tumor Growth. Cancer Res; 72(12); 2957–69.
| Cas No. | 607378-18-7 | SDF | |
| 化学名 | (Z)-2-((3r,5r,7r)-adamantan-1-yl)-N-((E)-2-((2-((2-hydroxyethyl)amino)ethyl)imino)-1,2-dihydroquinolin-5-yl)acetimidic acid dihydrochloride | ||
| Canonical SMILES | OCCNCC/N=C1C=CC2=C(N\1)C=CC=C2/N=C(O)/CC34C[C@@]5([H])C[C@](C3)([H])C[C@](C4)([H])C5.Cl.Cl | ||
| 分子式 | C25H34N4O2.2HCl | 分子量 | 495.48 |
| 溶解度 | <12.39mg/ml in Water; <49.55mg/ml in DMSO | 储存条件 | Desiccate at RT |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0182 mL | 10.0912 mL | 20.1824 mL |
| 5 mM | 0.4036 mL | 2.0182 mL | 4.0365 mL |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0182 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。