Hymeglusin
(Synonyms: Antibiotic 1233A) 目录号 : GC43883An HMG-CoA synthase inhibitor
Cas No.:29066-42-0
Sample solution is provided at 25 µL, 10mM.
Hymeglusin is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.[1][2] At a dose of 25 mg/kg, hymeglusin inhibits cholesterol biosynthesis in rats by 45%. Chiral studies indicate that the (2R,3R)-β-lactone moiety of hymeglusin is important for eliciting the specific inhibition of HMG-CoA synthase.[3] As a cell-wall targeting antibiotic, hymeglusin has been used to investigate the role of a gene important for controlling S. aureus virulence in a mouse sepsis model of infection.[4]
Reference:
[1]. Greenspan, M.D., Yudkovitz, J.B., Lo, C.Y., et al. Inhibition of hydroxymethylglutaryl-coenzyme A synthase by L-659,699. Proc. Natl. Acad. Sci. U.S.A. 84(21), 7488-7492 (1987).
[2]. Tomoda, H., Ohbayashi, N., Morikawa, Y., et al. Binding site for fungal β-lactone hymeglusin on cytosolic 3- hydroxy-3-methylglutaryl coenzyme A synthase. Biochim. Biophys. Acta 1636(1), 22-28 (2004).
[3]. Tomoda, H., Ohbayashi, N., Kumagai, H., et al. Differential inhibition of HMG-CoA synthase and pancreatic lipase by the specific chiral isomers of β-lactone DU-6622. Biochem. Bioph. Res. Commun. 265(2), 536-540 (1999).
[4]. Balibar, C.J., Shen, X., McGuire, D., et al. cwrA, a gene that specifically responds to cell wall damage in Staphylococcus aureus. Microbiology 156(Pt 5), 1372-1383 (2010).
Cas No. | 29066-42-0 | SDF | |
别名 | Antibiotic 1233A | ||
Canonical SMILES | OC[C@@H](C1=O)[C@H](O1)CCCC[C@@H](C)C/C(C)=C/C(C)=C/C(O)=O | ||
分子式 | C18H28O5 | 分子量 | 324.4 |
溶解度 | Soluble in ethanol, or in methanol, or in DMSO, or in chloroform | 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 | 3.0826 mL | 15.4131 mL | 30.8261 mL |
5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
10 mM | 0.3083 mL | 1.5413 mL | 3.0826 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。
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
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