Abafungin
(Synonyms: 阿巴芬净,BAY-W-6341) 目录号 : GC49766
An antifungal agent
Cas No.:129639-79-8
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
Abafungin is an antifungal agent.1 It is active against a variety of dermatophytes, yeast, molds, and other fungi (MICs = ≤0.06-2, 0.5-16, ≤0.06-1, and 0.25-8 µg/ml, respectively). Abafungin inhibits ergosterol biosynthesis, as well as acts directly on the fungal cell membrane to induce cell death.
1.Borelli, C., Schaller, M., Niewerth, M., et al.Modes of action of the new arylguanidine abafungin beyond interference with ergosterol biosynthesis and in vitro activity against medically important fungiChemotherapy54(4)245-259(2022)
| Cas No. | 129639-79-8 | SDF | Download SDF |
| 别名 | 阿巴芬净,BAY-W-6341 | ||
| Canonical SMILES | CC1=CC(C)=CC=C1OC2=C(C=CC=C2)C3=CSC(NC4=NCCCN4)=N3 | ||
| 分子式 | C21H22N4OS | 分子量 | 378.5 |
| 溶解度 | DMF: 10 mg/mL,DMSO: 2.5 mg/mL,Ethanol: 0.3 mg/mL,PBS (pH 7.2): 0.3 mg/mL | 储存条件 | -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 | 2.642 mL | 13.21 mL | 26.4201 mL |
| 5 mM | 0.5284 mL | 2.642 mL | 5.284 mL |
| 10 mM | 0.2642 mL | 1.321 mL | 2.642 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。
Modes of action of the new arylguanidine Abafungin beyond interference with ergosterol biosynthesis and in vitro activity against medically important fungi
Chemotherapy 2008;54(4):245-59.PMID:18587237DOI:10.1159/000142334.
Background: In contrast to the increasing numbers of agents for the treatment of invasive fungal infections, discoveries of new antifungal agents with therapeutic value in dermatomycoses are reported only rarely. Methods: Abafungin (chemical abstracts service registry No. 129639-79/8) is the first member of a novel class of synthetic antifungal compounds, the arylguanidines. It was first synthesized at Bayer AG, Leverkusen, Germany, and its antifungal action was discovered during the screening of H(2)-receptor antagonists based on the structure of famotidine. To obtain insight into its mode of action and antifungal activity, various tests were carried out with different fungal pathogens in vitro. Results: Abafungin was found to have potent antifungal activity. Furthermore, mode-of-action studies suggested that Abafungin exerts its antifungal activity regardless of whether the pathogens are growing or in a resting state. One target of Abafungin was found to be the inhibition of transmethylation at the C-24 position of the sterol side chain, catalyzed by the enzyme sterol-C-24-methyltransferase. A second action of Abafungin seems to be a direct effect on the fungal cell membrane. Conclusion: The observed characteristics of Abafungin indicate that Abafungin might be a promising antifungal agent defining a new class of antimycotics.
Bioactive thiazole and benzothiazole derivatives
Eur J Med Chem 2015 Jun 5;97:911-27.PMID:25455640DOI:10.1016/j.ejmech.2014.10.058.
The heterocycles are the versatile compounds existing in almost all natural products and synthetic organic compounds, usually associated with one or the other biological activity. Among the heterocycles the thiazoles and benzothiazoles occupy a prominent position. They possess a broad range of biological activities and are found in many potent biologically active molecules and drugs such as vitamin thiamine, sulfathiazol (antimicrobial drug), ritonavir (antiretroviral drug), Abafungin (antifungal drug) and tiazofurin (antineoplastic drug). The thiazole moiety is abundantly found in natural products while benzothiazole moiety is rare. In this review we disclose the literature reports of thiazoles and benzothiazoles possessing different biological activities.
Thiazole Containing Heterocycles with Antimalarial Activity
Curr Drug Discov Technol 2018;15(3):196-200.PMID:28745209DOI:10.2174/1570163814666170725114159.
Background: Heterocyclic compounds are the main class of medicinally important compounds. Many heterocyclic compounds bearing a five-membered ring in their structure have a good spectrum of biological activities. Thiazole is an important class of five-membered heterocyclic compounds. Thiazole and its derivatives exhibited a broad range of biological activities due to the presence of various reaction posseses. Thiazole, heterocyclic nucleus is present in several potent pharmacologically active molecules such as Sulfathiazole (antimicrobial drug), Ritonavir (antiretroviral drug), Tiazofurin (antineoplastic drug) and Abafungin (antifungal drug) etc. The search for some novel biologically active thiazoles is to be continued in the field of medicinal chemistry for investigators. An aim of this review is to identify and try making a SAR (Structure Activity Relationship) of substituted thiazole nucleus as possible new antimalarials. Method: Author undertook a structured search of bibliographic databases for peerreviewed research literature using a focused review question and inclusion/exclusion criteria. The quality of retrieved papers was appraised using standard tools. The characteristics of screened papers were described, and a deductive qualitative content analysis methodology was applied to analyse the interventions and findings of included studies using a conceptual framework. Result: Fifteen papers were included in the review; the majority were described about many biological activity of thiazole nucleus. Seven papers were find that had impacted upon the thaizoles as antimalarials. Some papers focused on the design, synthesis and antimalarial activity evaluation of thiazole derivatives. This review identified and made a SAR (Structure Activity Relationship) of substituted thiazole nucleus as possible new antimalarials. Conclusion: This review describes ongoing research in the search for novel thiazoles as targets and new antimalarial drug molecules.
Thiazole: A Review on Chemistry, Synthesis and Therapeutic Importance of its Derivatives
Curr Top Med Chem 2016;16(26):2841-2862.PMID:27150376DOI:10.2174/1568026616666160506130731.
Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place in medicinal chemistry. It is an essential core scaffold present in many natural (Vitamin B1- Thiamine) and synthetic medicinally important compounds. The versatility of thiazole nucleus demonstrated by the fact that it is an essential part of penicillin nucleus and some of its derivatives which have shown antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (Abafungin), antihistaminic and antithyroid activities. The synthetic importance of thiazole derivatives, its reduced forms and condensed derivatives have been increased much by their recent applications as anticancer (tiazofurin), anthelmintic, vulcanising accelerators (mercaptobenzothiazole) and photographic sensitizers. Thiazole chemistry has developed steadily after the pioneering work of Hofmann and Hantsch. Bogert and co-workers made significant contribution to expand this field. Mills established the importance of thiazole ring in cyanine dyes which is used as photographic sensitizer. Benzothiazole, a fused derivative of thiazole have also proved its commercial value. Present review describes chemical and biological importance of thiazole and its condensed derivatives with an emphasis on recent developments.
Gateways to clinical trials
Methods Find Exp Clin Pharmacol 2010 Jan-Feb;32(1):47-86.PMID:20383346doi
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