Neticonazole
(Synonyms: 奈康唑) 目录号 : GC39408
Neticonazole (SS717) is a selecvie inhibitor of exosome biogenesis and secretion. Neticonazole exhibits Neticonazole antifungal and antitumor activity.
Cas No.:130726-68-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.00%
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Neticonazole (SS717) is a selecvie inhibitor of exosome biogenesis and secretion. Neticonazole exhibits Neticonazole antifungal and antitumor activity.
Neticonazole treatment significantly reduces the Bcl-2/Bax ratio, leading to the restoration of the apoptosis level in xenograft tumors, which echoes the observation of inhibited tumor growth in neticonazole-treated IDB mice.[4]
[1] Amrita Datta, et al. Sci Rep. 2018 May 25;8(1):8161. [2] Sumiko Ishizaki, et al. Med Mycol J. 2019;60(4):91-94. [3] Lei Gu, et al. Invest New Drugs. 2020 Apr;38(2):221-228.
| Cas No. | 130726-68-0 | SDF | |
| 别名 | 奈康唑 | ||
| Canonical SMILES | CCCCCOC1=CC=CC=C1/C(N2C=CN=C2)=C\SC | ||
| 分子式 | C17H22N2OS | 分子量 | 302.43 |
| 溶解度 | DMSO: 250 mg/mL (826.64 mM) | 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 | 3.3066 mL | 16.5328 mL | 33.0655 mL |
| 5 mM | 0.6613 mL | 3.3066 mL | 6.6131 mL |
| 10 mM | 0.3307 mL | 1.6533 mL | 3.3066 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。
The exosome secretion inhibitor Neticonazole suppresses intestinal dysbacteriosis-induced tumorigenesis of colorectal cancer
Invest New Drugs 2020 Apr;38(2):221-228.PMID:30887254DOI:10.1007/s10637-019-00759-7.
Colorectal cancer (CRC) is the most frequently encountered malignancy associated with the rectum or colon, and accumulating evidences have implicated intestinal dysbacteriosis (IDB, disruption of gut microbiome) and exosomes in the pathology of CRC. We aimed to investigate the effect of IDB on exosome secretion in a CRC xenograft mouse model. An IDB mouse model was established and was inoculated with the CRC cell line SW480 as a xenograft tumor. Tumor growth was monitored for 15 days in sham and IDB mice, after which blood was collected to assess serum exosome secretion. A novel exosome secretion inhibitor, Neticonazole, was administered to IDB mice bearing CRC xenograft tumors, followed by monitoring of tumor growth and mouse survival. Western blot analysis was performed in xenograft tumors to investigate the underlying molecular mechanism. IDB promoted CRC xenograft tumor growth and exosome secretion, which could be inhibited by the exosome secretion inhibitor Neticonazole. Moreover, Neticonazole treatment significantly improved the survival of IDB mice with CRC xenograft tumors, likely through increasing apoptosis of CRC xenograft tumor cells. The exosome secretion inhibitor Neticonazole may serve as a promising therapeutic candidate against CRC by suppressing IDB-induced CRC tumorigenesis.
Effects of antifungal drugs on proliferation signals in Candida albicans
Biol Pharm Bull 2006 May;29(5):919-22.PMID:16651719DOI:10.1248/bpb.29.919.
The sensitivity of Candida albicans to antifungal drugs when cultured under aerobic and anaerobic conditions was measured. Ciclopirox olamine and siccanin were more effective under aerobic than under anaerobic conditions. Terbinafine, Neticonazole and amphotericin B showed the same antifungal activity under both aerobic and anaerobic conditions. None of these antifungal activities were affected by the pH conditions. Terbinafine inhibited the elongation of hyphae, while Neticonazole and amphotericin B induced proliferation of the yeast form. The expression of RAS1, EFG1 and CPH1 mRNAs was inhibited by these drugs. These results suggested that the inhibition of hyphal formation might be caused by disruption of the RAS1-signal pathway.
[Guidelines for diagnosis and treatment of mucocutaneous candidiasis]
Nihon Ishinkin Gakkai Zasshi 2009;50(4):207-12.PMID:19942790DOI:10.3314/jjmm.50.207.
This document summarizes current knowledge about diagnosis and treatment of candidiasis affecting the skin and oral mucosa. Several clinical forms of mucocutaneous candidiasis are distinguished depending on a patient's age and infected site, e.g. Candida intertrigo, erythema mycoticum infantile, erosio interdigitalis blastomycetica, candidal paronychia and onychia, Candida onychomycosis, and oral candidiasis. The diagnosis of candidiasis is confirmed by observation of mycelial forms on microscopic examination. Since Candida yeasts (especially C. albicans) are normal inhabitants of the skin and oral mucosa, it must always be noted that positive culture does not always indicate the presence of candidal infection. The pathogenicity of Candida species is relatively low, and some special conditions are required for tissue invasion by the fungus. Predisposing factors, such as disturbances of the cutaneous and mucosal microenvironment and systemic or local immunosuppression, should be checked in patients with recurrent infection. Therapy for cutaneous candidiasis is dominated by topical antifungal agents. Azole antifungal cream (e.g., bifonazole, ketoconazole, Neticonazole hydrochloride, lanoconazole and luliconazole) is most effective. Terbinafine hydrochloride and amorolfine hydrochloride are also useful. Cutaneous candidiasis usually requires a shorter duration of topical treatment (1-2 weeks) than superficial dermatophyte infections. For candidal paronychia and onychomycosis, oral therapy with itraconazole is recommended. The daily dose of itraconazole should be taken for several months, while its pulse therapy for candidiasis is not approved in Japan. Itraconazole oral solution is commonly used for oral candidiasis, and miconazole gel is also effective.
[Therapeutic efficacies of Neticonazole (SS717) cream and solution in experimental cutaneous Candida albicans infection of guinea pigs]
Jpn J Antibiot 1993 Oct;46(10):896-903.PMID:8254891doi
The therapeutic efficacies of 1% Neticonazole (SS717) cream and solution on experimental cutaneous Candida albicans infection produced in prednisolone-treated guinea pigs were compared with those of 1% bifonazole (BFZ). Active preparations or blank vehicles were applied once daily for 3 consecutive days starting 5 days postinfection. Therapeutic effects were assessed on the basis of viable counts recovered from the infected loci 9 days postinfection. In animals treated with SS 717 or BFZ cream, a significant mycological improvement was observed when compared to untreated controls. A significant therapeutic efficacy of a SS717 cream compared to cream vehicle was also noted, while there was no significant difference in the recovery of Candida between the untreated control group and the cream vehicle-treated groups. The mycological result of the SS717 solution treated group was significantly superior to those of the untreated control group, the solution vehicle-treated group and the BFZ solution-treated group. The treatment with a solution vehicle or a BFZ solution appeared to lower, though not to a significant level, viable counts at the infected loci. These results led us to the conclusion that both SS717 cream and solution preparations exhibited significantly superior activity to that of BFZ in experimental cutaneous candidasis of guinea pigs.
In vitro antifungal activities of luliconazole, a new topical imidazole
Med Mycol 2009;47(6):640-7.PMID:19115136DOI:10.1080/13693780802541518.
Luliconazole is a topical antifungal drug newly developed in Japan. The present study compares the in vitro antifungal activity of luliconazole against clinically important dermatomycotic fungi with that of other representative antifungal drugs. The reference drugs chosen were five classes of nine topical agents, i.e., allylamine (terbinafine), thiocarbamate (liranaftate), benzylamine (butenafine), morpholine (amorolfine), and azole (ketoconazole, clotrimazole, Neticonazole, miconazole and bifonazole). The minimum inhibitory concentrations (MIC) of luliconazole and the reference drugs against Trichophyton spp. (T. rubrum, T. mentagrophytes and T. tonsurans) and Candida albicans were measured by the standardized broth microdilution method. Luliconazole demonstrated greater potency against Trichophyton spp. (MIC range: