Liranaftate
The third generation of dithiocarbamate antifungal Toxicity Synthesis method Liranaftate cream Uses- Product Name
- Liranaftate
- CAS No.
- 88678-31-3
- Chemical Name
- Liranaftate
- Synonyms
- LNF;M-732;ZEFNART;LIRANAFATE;LIANAFTATE;LIRANAFTATE;PIRITETRATE;LIRANAFTATO;Liranaftatum;phthalenyl)ester
- CBNumber
- CB5168482
- Molecular Formula
- C18H20N2O2S
- Formula Weight
- 328.43
- MOL File
- 88678-31-3.mol
Liranaftate Property
- Melting point:
- 98.5-99.5°C
- Boiling point:
- 462.5±55.0 °C(Predicted)
- Density
- 1.240±0.06 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Sealed in dry,Room Temperature
- solubility
- DMSO (Slightly), Methanol (Slightly, Heated)
- form
- Solid
- pka
- 1.24±0.10(Predicted)
- color
- Off-White
- Merck
- 14,5515
Safety
- RTECS
- FD3890000
- HS Code
- 2933.39.4100
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H317May cause an allergic skin reaction
H319Causes serious eye irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P272Contaminated work clothing should not be allowed out of the workplace.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P363Wash contaminated clothing before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- L0301
- Product name
- Liranaftate
- Purity
- >98.0%(HPLC)
- Packaging
- 50mg
- Price
- $220
- Updated
- 2024/03/01
- Product number
- L0301
- Product name
- Liranaftate
- Purity
- >98.0%(HPLC)
- Packaging
- 250mg
- Price
- $761
- Updated
- 2024/03/01
- Product number
- L2637
- Product name
- Liranafate
- Packaging
- 10mg
- Price
- $403
- Updated
- 2021/12/16
- Product number
- L468850
- Product name
- Liranaftate
- Packaging
- 5mg
- Price
- $50
- Updated
- 2021/12/16
- Product number
- CS-2394
- Product name
- Liranaftate
- Purity
- 99.98%
- Packaging
- 10mg
- Price
- $96
- Updated
- 2021/12/16
Liranaftate Chemical Properties,Usage,Production
The third generation of dithiocarbamate antifungal
Liranaftate is a new king of third-generation dithiocarbamate antifungals , it is a new kind of the third category of chemicals,it belongs to squalene cyclooxygenase inhibitors, by inhibiting the fungal cell membrane squalene epoxidation reaction , it hinders the synthesis of ergosterol which is a constituent of cell membranes ,it plays the role of anti-fungal,its anti-fungal activity is 8 times of tolnaftate, and its dermatophytes effect is better than clotrimazole. It has a strong anti-fungal effect on skin filamentous fungi (Trichophyton,Microsporon, Epidermophyton) , it also shows antifungal activity on other filamentous fungi, dark fungi, dimorphic fungi.It is useful in the treatment of tinea capitis, ringworm, athlete's foot, tinea pedis, onychomycosis, tinea, jock itch, tinea versicolor and vulvovaginal candidiasis.
Toxicity
Reproductive toxicity: in general reproductive toxicity tests, subcutaneous administration to SD rats , the largest non-toxic dose for the parent is 20mg/kg, the largest non-toxic dose for the reproductive process and their pups is 100mg/kg.
Genetic Toxicity: Liranaftate mutagenicity tests are negative.
In toxicity tests during teratogenic sensitively period , subcutaneous administration ,the largest non-toxic dose of maternal is 300mg/kg, the largest non-toxic dose to fetal rats is100mg/kg.
In perinatal toxicity tests, administer subcutaneously, the largest non-toxic dose for the mother and newborn pups is 30mg/kg.
The above information is edited by the chemicalbook of Tian Ye.
Synthesis method
5,6,7,8-tetrahydro-2-naphthol reacts with thiophosgene to give the thio-5,6,7,8-tetrahydro-2-naphthyl chloroformate ester and 2-methoxy-6-methylamine pyridine, then react in isopropanol · water at room temperature for 2 hours to obtain liranaftate ,the overall yield is 70%.
Liranaftate cream
Liranaftate cream is a relatively safe topical antifungal formulation . In mutagenicity studies we found that no matter in chromosome aberration tests, or in the bone marrow micronucleus tests, Liranaftate cream has no effect on inducing cell chromosome aberrations , and it has no effect on bone marrow cell proliferation. It is used for the treatment of ringworm, athlete's foot, ringworm, jock itch, tinea versicolor and vulvovaginal candidiasis. Domestic manufacturers include: Chen Xin Shandong Lukang Pharmaceutical Co., Ltd. (Country medicine accurate words H20052287), Beijing Sihuan Pharmaceutical Technology Co., Ltd. Beijing Shengde Lai Bao Pharmaceutical Co., Ltd., Jiangsu zhongdan Pharmaceutical Co., Ltd.( Country medicine accurate words H20052733 ),Henan Tian Fang Pharmaceutical Co., Ltd. (Country medicine accurate words H20052552), and Nanjing Shenghe Pharmaceutical Co., Ltd. (Country medicine accurate words H20052554), Shideda Pharmaceutical (Beijing) Co., Ltd. (Country medicine accurate words H20052742), Kunshan Reddy pharmaceutical Co., Ltd. (Country medicine accurate words H20052345), Hugang Xinya pharmaceutical (Yangzhou) Co., Ltd. (Country medicine accurate words H20070143), Shandong Weigao pharmaceutical Co., Ltd. (Country medicine accurate words H20070073), Yangtze River pharmaceutical Group Co., Ltd. ( Country medicine accurate words H20080036), Heyuante Fukang pharmaceutical Co., Ltd. (Country medicine accurate words H20080162), Shandong Liangfu pharmaceutical Co., Ltd. (Country medicine accurate words H20080187)
Uses
Broad-spectrum antifungal
Description
Liranaftate was launched in Japan as a new topical antifungal for the treatment of dermatophycoses. This compound belonging to the thiocarbamate class of antifungals can be prepared by condensation of 5,6,7,8-tetrahydro-2-naphthol with the corresponding Npyridylthiocarbamoyl chloride. It is a potent and specific inhibitor of squalene epoxidase and consequently a blocker of ergosterol biosynthesis in fungi, without any detectable effect on mammalian cholesterol biosynthesis in rat liver at therapeutic dose levels. Liranaftate was found to be significantly more active than the other thiocarbamate tolnaftate against several dermatophytes, including Trichophyton mentagrophyfes, and against certain yeasts, such as Crypfococcus neoformans. On the other hand, it was inactive against a variety of Gram-positive and negative bacteria. When applicated as a 1 or 2% cream during clinical trials, it was well tolerated and no systemic absorption was observed.
Chemical Properties
White Crystalline Solid
Originator
Tosoh (Japan)
Uses
A squalene epoxidase inhibitor. Used as an antifungal.
Definition
ChEBI: Liranaftate is a member of tetralins.
brand name
Zefnart
Liranaftate Preparation Products And Raw materials
Raw materials
Preparation Products
Liranaftate Suppliers
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- United Kingdom
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View Lastest Price from Liranaftate manufacturers
- Product
- Liranaftate 88678-31-3
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 98%min
- Supply Ability
- 100KGS
- Release date
- 2023-05-15
- Product
- Liranaftate 88678-31-3
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100 MT
- Release date
- 2024-11-13
- Product
- Liranaftate 88678-31-3
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 50000KG/month
- Release date
- 2023-07-31