TunR1
目录号 : GC48213
An antibiotic and derivative of tunicamycin
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TunR1 is an antibiotic and derivative of tunicamycin .1 It is active against B. subtilis (MIC = 0.3 µg/ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G against B. subtilis when used at a concentration of 0.4 µg/ml. TunR1 (5 µg/ml) is cytotoxic to MDA-MB-231 breast cancer cells and non-cancerous CHO cells. Unlike tunicamycin, TunR1 does not inhibit glycosylation in a protein N-glycosylation assay.
1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)
| Cas No. | N/A | SDF | |
| Canonical SMILES | CC(N[C@H]1[C@@H](O[C@H]2[C@H](NC(CCCCCCCCCCC(C)C)=O)[C@@H](O)[C@@H](O)[C@@H](C[C@@H](O)[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C=CC(NC4=O)=O)O3)O2)O[C@H](CO)[C@@H](O)[C@@H]1O)=O.CC(N[C@H]5[C@@H](O[C@H]6[C@H](NC(CCCCCCCCCCCC(C)C)=O)[C@@H](O)[C@@H](O)[C@@H](C[C@@H](O)[C@@H]7[C@@H](O)[C@@H](O)[C@H](N8C=CC(NC8=O)=O)O7)O6)O[C@H](CO)[C@@H](O)[C@@H]5O)=O.CC(N[C@H]9[C@@H](O[C@H]%10[C@H](NC(CCCCCCCCCCCCC(C)C)=O)[C@@H](O)[C@@H](O)[C@@H](C[C@@H](O)[C@@H]%11[C@@H](O)[C@@H](O)[C@H](N%12C=CC(NC%12=O)=O)O%11)O%10)O[C@H](CO)[C@@H](O)[C@@H]9O)=O.CC(N[C@H]%13[C@@H](O[C@H]%14[C@H](NC(CCCCCCCCCCCCCC(C)C)=O)[C@@H](O)[C@@H](O)[C@@H](C[C@@H](O)[C@@H]%15[C@@H](O)[C@@H](O)[C@H](N%16C=CC(NC%16=O)=O)O%15)O%14)O[C@H](CO)[C@@H](O)[C@@H]%13O)=O | ||
| 分子式 | C39H66N4O16 (for TunR1 16:0) | 分子量 | 847 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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 | 1.1806 mL | 5.9032 mL | 11.8064 mL |
| 5 mM | 0.2361 mL | 1.1806 mL | 2.3613 mL |
| 10 mM | 0.1181 mL | 0.5903 mL | 1.1806 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。
Synergistic enhancement of beta-lactam antibiotics by modified tunicamycin analogs TunR1 and TunR2
J Antibiot (Tokyo) 2019 Nov;72(11):807-815.PMID:31420587DOI:10.1038/s41429-019-0220-x.
The β-lactams are the most widely used group of antibiotics in human health and agriculture, but this is under threat due to the persistent rise of pathogenic resistance. Several compounds, including tunicamycin (TUN), can enhance the antibacterial activity of the β-lactams to the extent of overcoming resistance, but the mammalian toxicity of TUN has precluded its use in this role. Selective hydrogenation of TUN produces modified compounds (TunR1 and TunR2), which retain the enhancement of β-lactams while having much lower mammalian toxicity. Here we show that TunR1 and TunR2 enhance the antibacterial activity of multiple β-lactam family members, including penems, cephems, and third-generation penicillins, to a similar extent as does the native TUN. Eleven of the β-lactams tested were enhanced from 2 to >256-fold against Bacillus subtilis, with comparable results against a penicillin G-resistant strain. The most significant enhancements were obtained with third-generation aminothiazolidyl cephems, including cefotaxime, ceftazidime, and cefquinome. These results support the potential of low toxicity tunicamycin analogs (TunR1 and TunR2) as clinically valid, synergistic enhancers for a broad group of β-lactam antibiotics.
Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactams
J Antibiot (Tokyo) 2017 Nov;70(11):1070-1077.PMID:28951601DOI:10.1038/ja.2017.101.
Tunicamycins (TUN) are inhibitors of the UDP-HexNAc: polyprenol-P HexNAc-1-P transferase family of enzymes, which initiate the biosynthesis of bacterial peptidoglycan and catalyze the first step in eukaryotic protein N-glycosylation. The TUN are therefore general and potent toxins to both eukaryotes and prokaryotes. Screening a library of synthetic TUN against Bacillus and yeast identified TUN that are antibacterial, but have significantly reduced eukaryotic toxicity. One of these (Tun-15:0) differs from the native TUN control only by the lack of the conjugated double bond in the tunicaminyl N-acyl group. Tun-15:0 also showed reduced inhibition for protein N-glycosylation in a Pichia-based bioassay. Natural TUN was subsequently modified by chemically reducing the N-acyl double bond (TunR1) or both the N-acyl and uridyl double bonds (TunR2). TunR1 and TunR2 retain their antibacterial activity, but with considerably reduced eukaryotic toxicity. In protein N-glycosylation bioassays, TunR1 is a less potent inhibitor than native TUN and TunR2 is entirely inactive. Importantly, the less toxic TunR1 and TunR2 both enhance the antibacterial activity of β-lactams: oxacillin by 32- to 64-fold, comparable with native TUN, and with similar enhancements for methicillin and penicillin G. Hence, the modified TUNs, TunR1 and TunR2, are potentially important as less-toxic synergistic enhancers of the β-lactams.