Liranaftate - CAS 88678-31-3
Catalog number: 88678-31-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H20N2O2S
Molecular Weight:
328.43
COA:
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Targets:
Antifungal
Description:
Liranaftate is a squalene epoxidase inhibitor exhabing anti-fungicidal activities.
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Purity:
>98%
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1.[Fungicidal activity of liranaftate against dermatophytes].
Oku Y1, Takahashi N, Yokoyama K. Nihon Ishinkin Gakkai Zasshi. 2009;50(1):9-13.
The fungicidal activities of the thiocarbamate antifungal agent liranaftate were compared to those of luliconazole, amorolfine hydrochloride and ketoconazole against twelve stock strains of three species of dermatophytes. The MICs of 0.001-0.009 microg/ml of luliconazole against Trichophyton rubrum (n=6)were the lowest among the agents tested, but its MCCs were considerably higher. Consequently, the antifungal potency of luliconazole was considered fungistatic. In contrast to this, the MCCs of 0.009-0.039 microg/ml of liranaftate against T. rubrum were the lowest and similar to its MICs. These results showed that liranaftate was fungicidal. All antifungals except ketoconazole tended to be fungicidal against both T. mentagrophytes (n=3)and Microsporum gypseum (n=3). In time-kill studies, liranaftate showed the greatest decrease to a below detection limit in viable counts of T. rubrum. The degree of killing of the strain by amorolfine was not greater than that seen by liranaftate, and little reduction of the viable counts by luliconazole and ketoconazole was observed irrespective of concentrations of the agents.
2.[Suppression of experimental inflammation by anti-fungal agent liranaftate in mice].
Maruyama N1, Abe Y, Hisajima T, Hayama K, Abe S. Nihon Ishinkin Gakkai Zasshi. 2010;51(1):7-11.
To evaluate the anti-inflammatory activity of the thiocarbamate antifungal agent liranaftate, the edema and the neutrophil accumulation detected by the activity of neutrophil marker enzyme, myeloperoxidase (MPO), were examined following application of liranaftate to mouse ears with inflammation induced by phorbol 12-myristate 13-acetate (PMA). Topical 20 microl administration of liranaftate in a dose-range between 1-4% suppressed the increase in ear thickness 6 hr after PMA application dose-dependently. Similarly, it decreased the weight increase of an ear section after 24 hr dose-dependently. More than 1% of liranaftate also suppressed augmentation of MPO activity of the ear section. This and histological observation indicate that liranaftate treatment suppressed neutrophil accumulation in PMA-applied ear lesion. From these results, we discussed that liranaftate might suppress inflammatory symptoms caused by trychophytosis in a clinical condition.
3.[Suppression of experimental footpad inflammatory reaction by anti-fungal agent liranaftate in mice].
Maruyama N1, Ishijima S, Abe S. Med Mycol J. 2012;53(2):129-33.
To evaluate the effect of the thiocarbamate antifungal agent liranaftate on inflammation and itchiness, footpad edema by phorbol 12-myristate 13-acetate (PMA) and the paw-licking accompanying by perceptual stimuli by compound 48/80 were examined. The effect of liranaftate application to mouse footpad on paw-licking time by compound 48/80 was observed. Topical administration of 4% liranaftate 1 hr before compound 48/80 did not suppress the paw-licking time, while pyrilamine, an anti-histamine agent, suppressed it significantly. As liranaftate was reported to suppress the ear inflammation induced by PMA, the effect of this agent on the footpad edema by PMA was examined. Liranaftate application significantly suppressed the increase in footpad swelling 24 hr after application of PMA, as true with ear inflammation. In this condition, we measured the paw-licking time by compound 48/80, but the suppression of time was not observed by the agent with or without the suppression of footpad inflammation.
4.[Fungicidal activity of liranaftate against Trichophyton rubrum].
Oku Y1, Sakuma K, Yokoyama K, Miyaji M. Nihon Ishinkin Gakkai Zasshi. 2002;43(3):181-7.
The fungicidal activities of thiocarbamate antifungal agent liranaftate were studied by determining the MIC and the MCC against Trichophyton rubrum with the Milliflex -100 Test System and by determining the time-kill curve in comparison to that of six reference agents. Liranaftate and lanoconazole both showed excellent fungistatic activity against the conidia of T. rubrum. For each of these agents, the MIC after 14 days of contact was 0.009 g/ml. The liranaftate-induced decrease in the MCC occurred from 9 days onwards; MCC at 14 days was 0.039 g/ml. The MCC for tolciclate was also reduced from 9 days onwards, but that of amorolfine, lanoconazole, neticonazole, clotrimazole and bifonazole was not lowered up to 14 days. Similar results were obtained when the studies were performed with germinated conidia. The time-kill curves showed that both liranaftate and tolciclate, at concentrations ranging from 2 to 32 times the MICs, achieved a decrease in viable counts to below the detection limit within 7 to 9 days.
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CAS 88678-31-3 Liranaftate

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