5-Benzyloxygramine
(Synonyms: 5-苄氧基芦竹碱) 目录号 : GC62808
5-Benzyloxygramine 是 N 蛋白、蛋白互作的原位稳定剂，具有抗病毒和稳定 N-NTD 蛋白的功能。
Cas No.:1453-97-0
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
5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities[1].
5-benzyloxygramine stabilizes the N-NTD dimers through simultaneous hydrophobic interactions with both partners, resulting in abnormal N protein oligomerization that was further confirmed in the cell[1].
[1]. Shan-Meng Lin, et al. Structure-Based Stabilization of Non-native Protein-Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design. J Med Chem. 2020 Mar 26;63(6):3131-3141.
| Cas No. | 1453-97-0 | SDF | |
| 别名 | 5-苄氧基芦竹碱 | ||
| 分子式 | C18H20N2O | 分子量 | 280.36 |
| 溶解度 | DMSO : 250 mg/mL (891.71 mM; Need ultrasonic) | 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 | 3.5668 mL | 17.8342 mL | 35.6684 mL |
| 5 mM | 0.7134 mL | 3.5668 mL | 7.1337 mL |
| 10 mM | 0.3567 mL | 1.7834 mL | 3.5668 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。
Actions of some analogues of 5-hydroxytryptamine on the isolated rat uterus and the rat fundus strip preparations
Br J Pharmacol Chemother 1959 Jun;14(2):265-72.PMID:13662587DOI:10.1111/j.1476-5381.1959.tb01397.x.
The search for substances which antagonize 5-hydroxytryptamine, and for those which act like it, has been extended to cover 5-substituted indoles which are analogues of 5-hydroxytryptamine, rather than analogues of tryptamine like the compounds previously studied by us. The isolated rat uterus and rat fundus strip preparations have been used to determine activity. The relationships between structure and activity of the compounds studied were not the same on the two preparations nor were they the same from one homologous series to another. These differences may be partly explained by the presence of amine oxidase in the rat fundus, as Vane (1959) has suggested, and by supposing that it is absent from the rat uterus. None of the compounds had marked antagonist activity. The most active antagonist on the rat uterus was 3-(2-aminopropyl)-5-benzyloxyindole, but this was less potent than 5-Benzyloxygramine. On the rat fundus strip, however, the only antagonist, 5-benzyloxy-3-(2-dimethylaminoethyl)indole, was more active than 5-Benzyloxygramine. On both preparations the most active stimulant was 3-(2-aminopropyl)-5-benzyloxyindole, which was about half as potent as 5-hydroxytryptamine. The next most active were 3-(2-aminopropyl)-5-methoxyindole and bufotenine.
Structure-Based Stabilization of Non-native Protein-Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design
J Med Chem 2020 Mar 26;63(6):3131-3141.PMID:32105468DOI:10.1021/acs.jmedchem.9b01913.
Structure-based stabilization of protein-protein interactions (PPIs) is a promising strategy for drug discovery. However, this approach has mainly focused on the stabilization of native PPIs, and non-native PPIs have received little consideration. Here, we identified a non-native interaction interface on the three-dimensional dimeric structure of the N-terminal domain of the MERS-CoV nucleocapsid protein (MERS-CoV N-NTD). The interface formed a conserved hydrophobic cavity suitable for targeted drug screening. By considering the hydrophobic complementarity during the virtual screening step, we identified 5-Benzyloxygramine as a new N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities. X-ray crystallography and small-angle X-ray scattering showed that 5-Benzyloxygramine stabilizes the N-NTD dimers through simultaneous hydrophobic interactions with both partners, resulting in abnormal N protein oligomerization that was further confirmed in the cell. This unique approach based on the identification and stabilization of non-native PPIs of N protein could be applied toward drug discovery against CoV diseases.
Two kinds of tryptamine receptor
Br J Pharmacol Chemother 1957 Sep;12(3):323-8.PMID:13460238DOI:10.1111/j.1476-5381.1957.tb00142.x.
There are two kinds of tryptamine receptor in the guinea-pig ileum, namely the M receptors which can be blocked with morphine and the D receptors which can be blocked with dibenzyline. Atropine, an atropine-like drug, cocaine, and methadone inhibit effects due to the M receptors, even after dibenzyline, but have no additional effect after morphine. Lysergic acid diethylamide, dihydroergotamine and 5-Benzyloxygramine inhibit effects due to the D receptors, even after morphine, but have no additional effect after dibenzyline. The M receptors are probably in the nervous tissue and the D receptors are probably in the muscles.
Actions of some analogues of tryptamine on the isolated rat uterus and on the isolated rat fundus strip preparations
Br J Pharmacol Chemother 1959 Mar;14(1):99-107.PMID:13651585DOI:10.1111/j.1476-5381.1959.tb00934.x.
Some 3-(2-dialkylaminoethyl)-, 3-(2-alkylaminoethyl)-, and 3-(2-dialkylaminoethyl)-2-methylindoles have been synthesized and tested, along with 5-Benzyloxygramine, 5-benzyloxy-3-(2-dimethylaminoethyl)-, 3-(2-aminopropyl)- and 3-(2-aminobutyl)-indoles, on the rat uterus and rat fundus strip. 5-Benzyloxy-3-(2-dimethylaminoethyl)indole, even though it contains an ethylene side-chain, was a less potent antagonist of 5-hydroxytryptamine than was 5-Benzyloxygramine. The remaining compounds were still less active. There are differences between the ability of some of them to antagonize 5-hydroxytryptamine and to antagonize tryptamine. 3-(2-Dimethylaminoethyl)-2-methylindole, in particular, shows a considerable degree of specific antagonism of 5-hydroxytryptamine on both tissues.Nearly all the compounds stimulate the preparations, some combining antagonism of 5-hydroxytryptamine at low concentrations with stimulant activity at higher concentrations. The most active compound is 3-(2-dipropylaminoethyl)indole. On the rat fundus strip this has, on a molar basis, 1/40th of the stimulant activity of 5-hydroxytryptamine, and is 20 times as active as tryptamine: on the rat uterus it is only 1/200th as active as 5-hydroxytryptamine, and equal in activity to tryptamine.
Two kinds of tryptamine receptor. 1957
Br J Pharmacol 1997 Feb;120(4 Suppl):134-9; discussion 132-3.PMID:9142401DOI:10.1111/j.1476-5381.1997.tb06789.x.
There are two kinds of tryptamine receptor in the guinea-pig ileum, namely the M receptors which can be blocked with morphine and the D receptors which can be blocked with dibenzyline. Atropine, an atropine-like drug, cocaine, and methadone inhibit effects due to the M receptors, even after dibenzyline, but have no additional effect after morphine. Lysergic acid diethylamide, dihydroergotamine and 5-Benzyloxygramine inhibit effects due to the D receptors, even after morphine, but have no additional effect after dibenzyline. The M receptors are probably in the nervous tissue and the D receptors are probably in the muscles.