RGH-5526 (GYKI-11679)
(Synonyms: GYKI-11679) 目录号 : GC32606
RGH-5526 (GYKI-11679) (GYKI-11679) 是一种新型抗高血压药物。
Cas No.:69579-13-1
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
Animal experiment: | Rats are used and treated with GYKI-11679 (0.5 mL of 1% Tween 80 suspension) at various dosages. They are killed at the specified times by decapitation; the heart is immediately removed, cut open, and rinsed in an isotonic saline solution. The brain is placed on ice and the hypothalamus is dissected. The tissues are weighed, homogenized in 5% trichloroacetic acid (TCA) containing 0.2% EDTA and ascorbic acid, and centrifuged for 1 h at 5000×g. The supernatant is processed on alumina and noradrenaline in the eluate is determined spectrofluorimetrically[1]. |
References: [1]. Huszti Z, et al. Influence on turnover and level of hypothalamic noradrenaline by a new antihypertensive agent (GYKI 11679). J Neurochem. 1981 Nov;37(5):1272-81. | |
GYKI-11679 is a new antihypertensive agent.
GYKI-11679 is a new antihypertensive agent. Results show a sharp (61%) reduction in the hypothalamic Noradrenaline (NA) level 2 h after the administration of 10 mg/kg of GYKI-11679, and this effect lasts for 4 to 6 h. It is demonstrated that GYKI-11679 exerts a greater NA lowering effect in the hypothalamus than in the periphery. GYKI-11679 does not influence the hypothalamic monoamine oxidase (MAO)-activity following prolonged treatment[1].
[1]. Huszti Z, et al. Influence on turnover and level of hypothalamic noradrenaline by a new antihypertensive agent (GYKI 11679). J Neurochem. 1981 Nov;37(5):1272-81.
| Cas No. | 69579-13-1 | SDF | |
| 别名 | GYKI-11679 | ||
| Canonical SMILES | C/C(CC(OC(C)(C)C)=O)=N\NC1=NN=C(N2CCOCC2)C=C1 | ||
| 分子式 | C16H25N5O3 | 分子量 | 335.4 |
| 溶解度 | Soluble in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL |
| 5 mM | 0.5963 mL | 2.9815 mL | 5.963 mL |
| 10 mM | 0.2982 mL | 1.4908 mL | 2.9815 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。
Sensitive method for the determination of 6-oxo-prostaglandin F1 alpha by gas chromatography with electron-capture and mass-fragmentographic detection
J Chromatogr 1986 Sep 19;365:161-9.PMID:3771702DOI:10.1016/s0021-9673(01)81553-3.
A selective and sensitive quantitative method is described for the determination of the endogenous prostacyclin content of the aorta of rats, treated with GYKI-11679, a new hydrazone derivative with antihypertensive action. The thoracal aorta from three rats was excised and pooled, 1 h after treatment with 10 mg/kg of GY-KI-11679. The prostacyclin, transformed to 6-oxo-PGF1 alpha, was extracted. For gas chromatographic electron-capture detection (GC-ECD), 6-oxo-PGF1 alpha was converted into the O-methyloxime tris(trifluoroacetyl) hexafluoroisopropyl ester derivative. The GC-ECD properties, stability and mass-spectrometric characteristics of this new derivative allow the quantitative analysis of 6-oxo-PGF1 alpha by using nor-PGF2 alpha as internal standard.
Preparation of new [1,2,4]triazolo[4,3-b]pyridazines. Part 12: Studies in the field of pyridazine compounds
Pharmazie 1983 Jun;38(6):369-71.PMID:6611639doi
6-Substituted-[1,2,4]triazolo[4,3-b]pyridazine-3-methanol, -aldehyde, -nitrile, -chloromethyl and -aminomethyl derivatives of potential antihypertensive activity were synthesized. The reduction of methyl[1,2,4]triazolo[4,3-b] pyridazine-3-carboxylate by lithium aluminium hydride and potassium borohydride was examined. The new compounds failed to exhibit hypotensive or antihypertensive effect. Compound 2a was a minor metabolite of GYKI-11679 [7].