Cannabidiol dimethyl ether
(Synonyms: CBDD,Cannabidiol-2',6'-dimethyl ether) 目录号 : GC13816
Pomalidomide - Peg2-azide is a synthetic E3 ligand -linker conjugate containing Pomalidomide based cereblon ligand and 2-unit PEG linker.
Cas No.:1242-67-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Pomalidomide - Peg2-azide is a synthetic E3 ligand -linker conjugate containing Pomalidomide based cereblon ligand and 2-unit PEG linker. PROTAC can be synthesized to target protein degradation[1].
The IC50 value of protac compound 21[(BRD4 BD1, IC50 = 41.8 nM) composed of Pomalidomide - Peg2-azide] was 0.81 µM in inhibiting THP-1 cell line growth. At the concentration of 1 µM, compound 21 can effectively degrade BRD4 protein and inhibit c-Myc[1].
References:
[1]. Zhang F, Wu Z, et,al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. doi: 10.1016/j.bmc.2019.115228. Epub 2019 Nov 30. PMID: 31813613.
| Cas No. | 1242-67-7 | SDF | |
| 别名 | CBDD,Cannabidiol-2',6'-dimethyl ether | ||
| 化学名 | 1,3-dimethoxy-2-[(1R,6R)-3-methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-benzene | ||
| Canonical SMILES | CCCCCc1cc(OC)c(c(OC)c1)[C@@H]1C=C(C)CCC1C(=C)C | ||
| 分子式 | C23H34O2 | 分子量 | 342.5 |
| 溶解度 | ≤14mg/ml in ethanol;1mg/ml in DMSO;2mg/ml in dimethyl formamide | 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。 |
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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 | 2.9197 mL | 14.5985 mL | 29.1971 mL |
| 5 mM | 0.5839 mL | 2.9197 mL | 5.8394 mL |
| 10 mM | 0.292 mL | 1.4599 mL | 2.9197 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。
In vivo and in vitro metabolism of cannabidiol monomethyl ether and cannabidiol dimethyl ether in the guinea pig: on the formation mechanism of cannabielsoin-type metabolite from cannabidiol
Oxidative metabolism of cannabidiol monomethyl ether (CBDM), one of the components of marihuana, was studied in the guinea pig. Cannabielsoin monomethyl ether (CBEM) was found to be formed with hepatic microsomes by gas chromatography-mass spectrometry (GC-MS). Experiments using various modifiers of enzymatic reaction suggested that, as in the case of cannabielsoin (CBE) formation from canabidiol (CBD), CBEM was formed from CBDM by the monooxygenase system including cytochrome P450. When cannabidiol dimethyl ether (CBDD), in which phenolic hydroxyl groups of CBD are masked with methyl groups, was incubated with liver microsomes and an reduced nicotinamide adenine dinucleotide phosphate-generating system, 1S,2R-epoxy-CBDD was identified by GC-MS. The epoxy metabolite was also found in the liver of a guinea pig pretreated with CBDD (100 mg/kg, intraperitoneally) 1 h before sacrifice. Rate of 1S,2R-epoxide metabolism was slower than that of 1R,2S-epoxy-CBDD under the conditions, as in the microsomal oxidation of CBDD described above. These results indicate that 1S,2R-epoxides are formed from CBD, CBDM and CBDD and that the epoxides are quickly converted to elsoin-type metabolites in the cases of CBD and CBDM.