Harmalol hydrochloride
(Synonyms: 盐酸骆驼蓬酚) 目录号 : GC60894
A β-carboline alkaloid and an active metabolite of harmaline
Cas No.:6028-07-5
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
Harmalol is a β-carboline alkaloid and an active metabolite of harmaline that has been found in P. harmala and has diverse biological activities.1,2,3,4,5 It is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A; IC50 = 0.63 ?M) and monoamine oxidase A (MAO-A; IC50 = 0.66 ?M).3 It is selective for DYRK1A over Cdk1, Cdk5, CK1α1, Clk4, DYRK2, Pim-1, and GSK3β but also inhibits DYRK1B and Clk1 at 10 ?M. It inhibits proliferation of H4 human glioblastoma cells (IC50s = 23.7 ?M). Harmalol (0.5-12.5 ?M) reduces increases in the levels of the cytochrome P450 (CYP) isoform CYP1A1 induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in HepG2 cells and prevents TCDD-induced activation of the aryl hydrocarbon receptor (AhR) in guinea pig hepatic cytosolic extracts.4 It reduces glutamate-induced cytotoxicity, cytochrome c release, caspase-3 activation, and the production of reactive oxygen species (ROS) in PC12 cells when used at a concentration of 25 ?M.5 This product is also available as an analytical reference standard .
1.Brierley, D.I., and Davidson, C.Developments in harmine pharmacology – implications for ayahuasca use and drug-dependence treatmentProg. Neuropsychopharmacol. Biol. Psychiatry39(2)263-272(2012) 2.Nikam, T.D., Nitnaware, K.M., and Ahire, M.L.Alkaloids derived from tryptophan: Harmine and related alkaloidsNatural products. Phytochemistry, botany and metabolism of alkaloids, phenolics and terpenes553-574(2013) 3.Tarpley, M., Oladapo, H.O., Strepay, D., et al.Identification of harmine and β-carboline analogs from a high-throughput screen of an approved drug collection; profiling as differential inhibitors of DYRK1A and monoamine oxidase A and for in vitro and in vivo anti-cancer studiesEur. J. Pharm. Sci.162105821(2021) 4.El Gendy, M.A.M., Soshilov, A.A., Denison, M.S., et al.Harmaline and harmalol inhibit the carcinogen-activating enzyme CYP1A1 via transcriptional and posttranslational mechanismsFood Chem. Toxicol.50(2)353-362(2012) 5.Han, E.S., and Lee, C.S.Inhibition of glutamate-induced change in mitochondrial membrane permeability in PC12 cells by 1-methylated β-carbolinesBiomol. Ther. (Seoul)11(2)112-118(2003)
| Cas No. | 6028-07-5 | SDF | |
| 别名 | 盐酸骆驼蓬酚 | ||
| Canonical SMILES | CC1=NCCC2=C1NC3=C2C=CC(O)=C3.[H]Cl | ||
| 分子式 | C12H13ClN2O | 分子量 | 236.7 |
| 溶解度 | 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 | 4.2248 mL | 21.1238 mL | 42.2476 mL |
| 5 mM | 0.845 mL | 4.2248 mL | 8.4495 mL |
| 10 mM | 0.4225 mL | 2.1124 mL | 4.2248 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。
Comparative Therapeutic Effects of Natural Compounds Against Saprolegnia spp. (Oomycota) and Amyloodinium ocellatum (Dinophyceae)
Front Vet Sci 2020 Feb 21;7:83.PMID:32154278DOI:10.3389/fvets.2020.00083.
The fish parasites Saprolegnia spp. (Oomycota) and Amyloodinium ocellatum (Dinophyceae) cause important losses in freshwater and marine aquaculture industry, respectively. The possible adverse effects of compounds used to control these parasites in aquaculture resulted in increased interest on the search for natural products with antiparasitic activity. In this work, eighteen plant-derived compounds (2',4'-Dihydroxychalcone; 7-Hydroxyflavone; Artemisinin; Camphor (1R); Diallyl sulfide; Esculetin; Eucalyptol; Garlicin 80%; Harmalol hydrochloride dihydrate; Palmatine chloride; Piperine; Plumbagin; Resveratrol; Rosmarinic acid; Sclareolide; Tomatine, Umbelliferone, and Usnic Acid) have been tested in vitro. Sixteen of these were used to determine their effects on the gill cell line G1B (ATCC®CRL-2536™) and on the motility of viable dinospores of Amyloodinium ocellatum, and thirteen were screened for inhibitory activity against Saprolegnia spp. The cytotoxicity results on G1B cells determined that only two compounds (2',4'-Dihydroxychalcone and Tomatine) exhibited dose-dependent toxic effects. The highest surveyed concentrations (0.1 and 0.01 mM) reduced cell viability by 80%. Upon lowering the compound concentration the percentage of dead cells was lower than 20%. The same two compounds revealed to be potential antiparasitics by reducing in a dose-dependent manner the motility of A. ocellatum dinospores up to 100%. With respect to Saprolegnia, a Minimum Inhibitory Concentration was found for Tomatine (0.1 mM), Piperine and Plumbagin (0.25 mM), while 2',4'-Dihydroxychalcone considerably slowed down mycelial growth for 24 h at a concentration of 0.1 mM. Therefore, this research allowed to identify two compounds, Tomatine and 2',4'-Dihydroxychalcone, effective against both parasites. These compounds could represent promising candidates for the treatment of amyloodiniosis and saprolegniosis in aquaculture. Nevertheless, further in vitro and in vivo tests are required in order to determine concentrations that are effective against the considered pathogens but at the same time safe for hosts, environment and consumers.