规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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靶点 |
5-HT2A Receptor (Ki = 397 nM); DYRK1A
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体外研究 (In Vitro) |
Harmine 通过特定 DANDY 抑制 DYRK1A 的 tau 磷酸化,IC50 为 190 nM[2]。 Harmine 通过破坏 Rad51 募集而对肝癌细胞产生极端的细胞毒性,从而负向调节同源重组 (HR)。此外,当暴露于 NHEJ 抑制剂 Nu7441 时,Hep3B 细胞更容易受到去氢骆驼蓬碱的抗增殖作用的影响[3]。
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体内研究 (In Vivo) |
研究表明,TBI组的脑含水量明显较高。与 TBI 组相比,去氢骆驼蓬碱治疗在 1、3 和 5 天时显着降低了组织含水量。将 3 天和 5 天的逃避潜伏期与 TBI 组进行比较时,使用氨胺治疗显着降低了逃避潜伏期。与未接受Harmine治疗的TBI组相比,在TBI后1、3和5天给予Harmine后,大鼠的运动功能恢复得到显着改善。与TBI组相比,去氢骆驼蓬碱治疗组的神经元存活率明显更高。当给予Harmine时,与TBI组相比,GLT-1表达显着增加。与 TBI 组相反,给予去氢骆驼蓬碱可显着降低 caspase 3 的表达[4]。
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细胞实验 |
DNA 损伤、细胞死亡和增殖实验均采用高内涵筛选 (HCS) 形式进行。使用涂有 100 µg/mL 聚-L-鸟氨酸和 10 µg/mL 层粘连蛋白的多孔 384 µClear 板来镀 hNPC(1,500 个细胞/每孔)。 24 小时后,在补充有 bFGF 和 EGF 的 N2B27 培养基中,用去氢骆驼蓬碱、INDY 和帕吉林处理细胞五次(每个条件 5 个孔),持续四天。第 4 天:固定或图像采集前 30 分钟,用 10 µM EdU 标记细胞进行细胞增殖,用 BOBO™ -3 进行细胞死亡标记。
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动物实验 |
Rats: The study uses 150 male Sprague-Dawley rats, weighing between 280 and 320 g and aged between 10 and 12 weeks. Three groups of rats are randomly assigned: the TBI group (n=35); the TBI + Harmine-treated group (n=35); and the Sham-operated group (n= 15). Immediately after traumatic brain injury, heroine (i.p., 30 mg/kg daily) is given for a maximum of five days. Equal volumes of 0.9% saline solution are given to the TBI and sham groups (i.p.). For the purpose of examining behavioral recovery, the rats are divided into three groups: Sham (n = 3), TBI (n = 7), and Harmine (n = 7). The NSS is assessed 1, 3, and 5 days after a traumatic brain injury. An observer who is blind to the animal treatment evaluates each rat individually[4].
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参考文献 |
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分子式 |
C13H12N2O
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分子量 |
212.2472
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精确质量 |
212.10
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元素分析 |
C, 73.56; H, 5.70; N, 13.20; O, 7.54
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CAS号 |
442-51-3
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相关CAS号 |
Harmine hydrochloride;343-27-1
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外观&性状 |
Solid powder
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SMILES |
CC1=NC=CC2=C1NC3=C2C=CC(=C3)OC
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InChi Key |
BXNJHAXVSOCGBA-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C13H12N2O/c1-8-13-11(5-6-14-8)10-4-3-9(16-2)7-12(10)15-13/h3-7,15H,1-2H3
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化学名 |
7-methoxy-1-methyl-9H-pyrido[3,4-b]indole
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别名 |
Harmine; telepathine; Yageine; Yajeine; Banisterine; Leucoharmine
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: ≥ 30 mg/mL (~141.3 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 4.7114 mL | 23.5571 mL | 47.1143 mL | |
5 mM | 0.9423 mL | 4.7114 mL | 9.4229 mL | |
10 mM | 0.4711 mL | 2.3557 mL | 4.7114 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05526430 | Completed | Drug: Harmine Hydrochloride Capsules |
Diabetes Mellitus | James Murrough | September 13, 2022 | Phase 1 |
NCT04716335 | Completed | Drug: DMT Drug: Harmine |
Emotions Mood |
Psychiatric University Hospital, Zurich |
December 1, 2020 | Early Phase 1 |
NCT05780216 | Completed | Drug: DMT + harmine Drug: Placebo |
Healthy Participants | Milan Scheidegger | February 20, 2023 | Early Phase 1 |
In vitro inhibition of a panel of 13 kinases by F-DANDYs 5a and 5g (5.10−8 M) and harmine (10−6 M) (100 represents full inhibition of the enzyme). td> |
Harmine inhibits the efficiency of HR and suppresses the proliferation in Hep3B and HuH7 cells. Cancer Biol Ther . 2015;16(11):1585-92. td> |
Harmine blocks HR by inhibiting Rad51 recruitment. Cancer Biol Ther . 2015;16(11):1585-92. td> |
Harmine induces S and G2/M phase arrest in Hep3B cells in an ATM and ATR dependent manner. Cancer Biol Ther . 2015;16(11):1585-92. td> |
Effects of harmine on escape latency performance at 1, 3 and 5 days (d). Mol Med Rep . 2015 Dec;12(6):7985-91. td> |
Effects of harmine on the survival rates of neurons in the hippocampal region at 24 h. Mol Med Rep . 2015 Dec;12(6):7985-91. td> |