CUMYL-CH-MeGACLONE
目录号 : GC47133
A neuropeptide with diverse biological activities
Cas No.:2813950-07-9
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
CUMYL-CH-MeGACLONE is an analytical reference standard categorized as a synthetic cannabinoid.1 This product is intended for research and forensic applications.
1.Haschimi, B., Giorgetti, A., Mogler, L., et al.The novel psychoactive substance Cumyl-CH-MEGACLONE: Human phase-I metabolism, basic pharmacological characterization, and comparison to other synthetic cannabinoid receptor agonists with a γ-carboline-1-one coreJ. Anal. Toxicol.bkaa065(2020)
| Cas No. | 2813950-07-9 | SDF | |
| Canonical SMILES | CC(C1=CC=CC=C1)(C)N2C=CC(N(CC3CCCCC3)C4=C5C=CC=C4)=C5C2=O | ||
| 分子式 | C27H30N2O | 分子量 | 398.5 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml | 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 | 2.5094 mL | 12.5471 mL | 25.0941 mL |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 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。
The Novel Psychoactive Substance CUMYL-CH-MeGACLONE: Human Phase-I Metabolism, Basic Pharmacological Characterization and Comparison to Other Synthetic Cannabinoid Receptor Agonists with a γ-Carboline-1-One Core
J Anal Toxicol 2021 Mar 12;45(3):277-290.PMID:32514544DOI:10.1093/jat/bkaa065.
Synthetic cannabinoids (SC) remain one of the largest groups of new psychoactive substances on the European drug market. In December 2018, CUMYL-CH-MeGACLONE, a novel SC based on a γ-carboline-1-one core structure, was firstly identified in Hungary and later also other European countries. This work aims to reveal the pharmacological characteristics and phase-I metabolism of CUMYL-CH-MeGACLONE and compare the data to its analogs Cumyl-PEGACLONE and 5F-Cumyl-PEGACLONE. The purified substance was characterized by means of gas chromatography-mass spectrometry (GC-MS), liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-QToF-MS), attenuated total reflection infrared spectroscopy (ATR-FTIR) and nuclear magnetic resonance spectroscopy. Phase-I metabolites were identified by LC-QToF-MS analysis combined with a scheduled precursor ion list of authentic urine samples and confirmed by comparison with metabolites built in vitro by pooled human liver microsome assays. Pharmacological data were obtained in a competitive ligand binding assay and a receptor activation assay at the human cannabinoid receptor 1 (hCB1). The structure of 5-cyclohexylmethyl-2-(2-phenylpropan-2-yl)-2,5-dihydro-1H-pyrido[4,3-b]indol-1-one (semisystematic name: CUMYL-CH-MeGACLONE) was identified in a herbal blend as the main active ingredient. Investigation of phase-I biotransformation of CUMYL-CH-MeGACLONE led to three monohydroxylated metabolites (M08, M10 and M13) as reliable urinary markers for proof of consumption. At the hCB1, CUMYL-CH-MeGACLONE shows high binding affinity with Ki = 1.01 nM (2.5-fold higher than JWH-018), an EC50 of 1.22 nM and high efficacy with EMAX = 143.4% above constitutive activity of the receptor (1.13-fold higher than JWH-018). Comparison to the analogs 5F-Cumyl-PEGACLONE and Cumyl-PEGACLONE (both are hCB1 full agonists carrying a 5-fluoropentyl or pentyl chain instead of the cyclohexylmethyl moiety) suggests that CUMYL-CH-MeGACLONE is more likely to resemble the pharmacologic profile of the latter one.
Clinical symptoms and blood concentration of new psychoactive substances (NPS) in intoxicated and hospitalized patients in the Budapest region of Hungary (2018-19)
Clin Toxicol (Phila) 2022 Jan;60(1):18-24.PMID:34080493DOI:10.1080/15563650.2021.1928162.
Background: New Psychoactive Substances (NPS) impose a new challenge on the legal and health care system, yet, there is little information available about how new substances spread based on hospitalization of intoxicated patients. The aims of this study were: (i) to investigate the frequency of NPS among suspected drug intoxicated patients, (ii) to study the connection between blood concentration and clinical symptoms, (iii) to determine their half-life with a time-series blood sampling protocol. Methods: During the observation period, 116 suspected drug intoxicated patients were sampled. The samples were analyzed for alcohol, 20 classical illicit and licit drugs, and for 78 NPS. Clinical symptoms were registered on-site (by the Emergency Medical Services) and (also) at hospital admittance. Results: NPS were detected in 51 patients of which cathinones were found in 4, the synthetic cannabinoids (SCs) 5 F-MDMB-PINACA and 5 F-MDMB-PICA in 23-23, and CUMYL-CH-MeGACLONE in 2 cases. Poison severity scores (PSS) showed mild to moderate intoxications overall. Connection between blood concentration and severity of clinical symptoms were inconclusive. The calculated half-life of 5 F-MDMB-PINACA and 5 F-MDMB-PICA was 2.50 and 2.68 h, respectively. Conclusion: The ratio of SCs among the selected intoxicated patients was higher than expected from seizure data which could be the consequence of targeted patient selection. The clinical symptoms and the severity of intoxication cannot be characterized simply by NPS blood levels. The short half-life of SCs can explain the relatively rapid consolidation of intoxication symptoms.HighlightsIn the Budapest region, the majority of hospitalized NPS intoxications was caused by the synthetic cannabinoids 5F-MDMB-PINACA and 5F-MDMB-PICA in 2018-19.No correlation between blood concentration and symptoms severity could be established.The clinical symptoms of synthetic cannabinoid users improved quickly and no ICU treatment was necessary.The half-life of 5F-MDMB-PINACA and 5F-MDMB-PICA was proved to be 2.50 hours and 2.68 hours, respectively.