Kifunensine
(Synonyms: 几夫碱,FR900494) 目录号 : GC17735An inhibitor of glycoprotein biosynthesis
Cas No.:109944-15-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kifunensine was originally isolated from the actinomycete Kitasatosporia kifunensine No. 9482 and shown to be a weak inhibitor of aryl mannosidase.[1],[2] It has since been shown to be a potent and selective inhibitor of class I α-mannosidases and may serve as a key inhibitor of glycoprotein biosynthesis.[3] Kifunensine inhibits both human endoplasmic reticulum α-1,2-mannosidase I and members of the Golgi subfamily of the class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively. It also inhibits mung bean α-1,2-mannosidase I with an IC50 value of 20-50 nM.3 Kifunensine can be used to block α-mannosidase I activity at the endoplasmic reticulum (ER), preventing the removal of desired mutated proteins through ER quality control mechanisms.[4],[5]
Reference:
[1]. Iwami, M., Nakayama, O., Terano, H., et al. A new immunomodulator, FR-900494: Taxonomy, fermentation, isolation, and physico-chemical and biological characteristics. Journal of Antibiotics XL(5), 612-622 (1987).
[2]. Kayakiri, H., Takase, S., Shibata, T., et al. Structure of kifunensine, a new immunomodulator isolated from an actinomycete. The Journal of Organic Chemistry 54, 4015-4016 (1989).
[3]. Hering, K.W., Karaveg, K., Moremen, K.W., et al. A practical synthesis of kifunensine analogues as inhibitors of endoplasmic reticulum α-mannosidase I. The Journal of Organic Chemistry 70, 9892-9904 (2005).
[4]. Bartoli, M., Gicquel, E., Barrault, L., et al. Mannosidase I inhibition rescues the human α-sarcoglycan R77C recurrent mutation. Human Molecular Genetics 17(9), 1214-1221 (2008).
[5]. Soheili, T., Gicquel, E., Poupiot, J., et al. Rescue of sarcoglycan mutations by inhibition of endoplasmic reticulum quality control is associated with minimal structural modifications. Human Mutation 33(2), 429-439 (2012).
Cas No. | 109944-15-2 | SDF | |
别名 | 几夫碱,FR900494 | ||
化学名 | (hexahydro-6R,7S,8aS-trihydroxy-5R-(hydroxymethyl)-imidazo[1,2-a]pyridine-2,3-dione | ||
Canonical SMILES | VO[C@@H]([C@H]1O)[C@@H](NC2=O)N(C2=O)[C@H](CO)[C@H]1O | ||
分子式 | C8H12N2O6 | 分子量 | 232.19 |
溶解度 | DMSO : 11.9 mg/mL (51.25 mM; Need ultrasonic);0.5mg/mL in warm distilled water | 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 | 4.3068 mL | 21.5341 mL | 43.0682 mL |
5 mM | 0.8614 mL | 4.3068 mL | 8.6136 mL |
10 mM | 0.4307 mL | 2.1534 mL | 4.3068 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。