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Olorofim

Catalog No. T27300 CAS 1928707-56-5

Synonyms: Olorofim, F901318, F-901318

Olorofim is a novel selective antifungal compound with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM) and almost no inhibitory effect on human DHODH (<100 uM).Olorofim has good efficacy against various pathogenic filamentous and dimorphic fungi such as Penicillium spp, Dermatophilus spp and Fusarium spp.

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Olorofim, CAS 1928707-56-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 390.00
5 mg	In stock	$ 927.00
10 mg	In stock	$ 1,260.00
25 mg	In stock	$ 1,850.00
50 mg	In stock	$ 2,280.00
100 mg	In stock	$ 2,800.00

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Purity: 99.28%

Biological Description

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Description	Olorofim is a novel selective antifungal compound with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM) and almost no inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against various pathogenic filamentous and dimorphic fungi such as Penicillium spp, Dermatophilus spp and Fusarium spp.
Targets&IC50	Talaromyces species/Trichophyton species:0.015 mg/L(MIC), Penicillium:0.027 mg/L(MIC), Cryptic aspergillis:0.004-0.03 mg/L(MIC), Trichophyton isolates:0.008 mg/L(MIC), Dermatophytes and opportunistic moulds:0.004-0.125 mg/L(MIC)
In vitro	Olorofim (0.004-0.125 mg/L) showed highly potent in vitro activity against dermatophytes and opportunistic moulds (MIC range of 0.004-0.125 mg/L) except for Alternaria alternata. Penicillium, and Talaromyces species and Trichophyton species exhibited a low geometric mean (GM) MIC (GM 0.027 mg/L and 0.015 mg/L, respectively) of olorofim. Importantly, a 2-12 dilution step decrease in in vitro activity of olorofim as compared with azoles was observed against Penicillium and Talaromyces. Notably, olorofim displayed potent in vitro activity against Trichophyton isolates including terbinafine-resistant and azole-resistant Trichophyton mentagrophytes/interdigitale with a modal MIC value of 0.008 mg/L. Further, azole-resistant A. fumigatus isolates harbouring mutations in azole target Cyp51A genes and several cryptic aspergilli displayed low MICs (range 0.004-0.03 mg/L) of olorofim.[2]
In vivo	The in vivo efficacy of the drug was investigated, using a guinea pig model, experimentally infected with Microsporum gypseum. Typical skin lesions of dermatophyte infection were observed in the guinea pig model at 7 days postinoculation. Following 1 week of daily topical administration of olorofim, similar to the clotrimazole group, the skin lesions were resolved and normal hair growth patterns appeared.[1]

Synonyms	Olorofim, F901318, F-901318
Molecular Weight	498.55
Formula	C28H27FN6O2
CAS No.	1928707-56-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (100.29 mM)

References and Literature

1. Mirbzadeh Ardakani E, et al. Olorofim Effectively Eradicates Dermatophytes In Vitro and In Vivo. Antimicrob Agents Chemother. 2021;65(12):e0138621. 2. Oliver JD, Sibley GE, Beckmann N, Dobb KS, Slater MJ, McEntee L, du Pré S, Livermore J, Bromley MJ, Wiederhold NP, Hope WW, Kennedy AJ, Law D, Birch M. F901318 represents a novel class of antifungal drug that inhibits dihydroorotate dehydrogenase. Proc Natl Acad Sci U S A. 2016 Oct 25. pii: 201608304. [Epub ahead of print] PubMed PMID: 27791100; PubMed Central PMCID: PMC5111691. 3. Singh A, et al. In vitro activity of the novel antifungal olorofim against dermatophytes and opportunistic moulds including Penicillium and Talaromyces species. J Antimicrob Chemother. 2021;76(5):1229-1233. 4. Lim W, et al. Madurella mycetomatis, the main causative agent of eumycetoma, is highly susceptible to olorofim. J Antimicrob Chemother. 2020;75(4):936-941.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Mitochondria-Targeted Compound Library Clinical Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Olorofim 1928707-56-5 F901318 F 901318 F-901318 inhibitor inhibit

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