Product Details
| Product Name:
Olorofim |
CAS No.:
1928707-56-5 |
| Purity:
99.28% |
Supply Ability:
10g |
| Release date:
2024/11/06 |
Product Introduction
Bioactivity
| 名稱 | Olorofim |
| 描述 | Olorofim（F-901318）is a novel selective antifungal compound targeting pyrimidine biosynthesis in mycobacteria, with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM), but little inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against a variety of pathogenic filamentous and dimorphic fungi, such as Penicillium spp, P. dermatitidis spp and Fusarium spp. |
| 體外活性 | METHODS: 10 4 spores were suspended in 80 μl RPMI 1640 medium, buffered to pH 7.0 (with MOPS) and inoculated into 96-well microtiter plates. Then 20 μ Olorofim (F-901318) 0.0001-1 μg/ml was added to each well and the plates were incubated at 28°C. MICs were assessed by microtiter after 96 h of incubation.
RESULTS Dermatophytes were highly susceptible to Olorofim in vitro (MIC = 0.015–0.06 mg/L). [1]
METHODS: Olorofim was used to determine the in vitro antifungal activity of 246 azole-susceptible A. fumigatus isolates, 5 A. fumigatus isolates with TR34/L98H-mediated resistance, 19 Rhizopus isolates, 21 Fusarium species isolates, and one isolate each of 6 other fungi.
RESULTS Olorofim showed consistent antifungal activity against azole-susceptible A. fumigatus isolates (MIC50 = 0.008 μg/mL); all A. fumigatus isolates fell within the one- to two-fold dilution range of the MIC50 (0.008 μg/mL); five azole-resistant A. fumigatus isolates with Cyp51A-associated point mutations had MIC values ??of 0.008 μg/mL. [3] |
| 體內(nèi)活性 | METHODS: A guinea pig model of dermatophytosis was established. Starting from the eighth day after infection, Olorofim（F-901318） (0.1 mg/ml in PEG300) was topically applied every day at a dose of 10 μg/lesion site for 7 days.
RESULTS Skin lesions resolved and normal hair growth pattern occurred. [1]
METHODS: Cyclophosphamide-immunosuppressed CD-1 mice infected with Scedosporium apiospermum, Pseudallescheria boydii (Scedosporium boydii), and Lomentospora prolificans were treated with intraperitoneal administration of olorofim (15 mg/kg every 8 hours for 9 days). The efficacy of olorofim treatment was assessed by survival 10 days post-infection, serum (1-3)-β-d-glucan (BG) levels 3 days post-infection, histopathology, and renal fungal burden.
RESULTS In olorofim-treated mice, serum BG levels were significantly suppressed, fungal DNA detected in target organs was significantly lower than in controls, and no or only a few bands were observed in histopathological observations of mouse kidneys. Lesions with hyphal elements. [2] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (100.29 mM)
|
| 關(guān)鍵字 | F 901318 |
| 相關(guān)產(chǎn)品 | Dehydroacetic acid sodium | 2-Butyl-1,2-benzisothiazolin-3-one | Tebuconazole | Potassium gluconate | Chitosan (MW 150000) | Rotenone | Veratraldehyde | Paclobutrazol | Lauryl betaine | Potassium sorbate | Geraniol | Isomalt |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌細胞代謝庫 | 抗真菌庫 | 藥物功能重定位化合物庫 | 線粒體靶向庫 | 臨床期小分子藥物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States