Buy High purity Efinaconazole good producer CAS NO.164650-44-6

Buy High purity Efinaconazole good producer

In October 2013, efinaconazole (also known as KP-103) was approved in Canada as a 10% topical solution for the treatment of onychomycosis. Like other azole antifungal agents, efinaconazole acts by disrupting fungal cell membranes through inhibition of sterol 14α-demethylase, an enzyme involved in the biosynthesis of ergosterol, which is a key component of the fungal cell membrane. Efinaconazole has potent antifungal activity against clinical isolates of dermatophytes, including Trichophyton mentagrophyes (MIC₈₀ =0.125 μg/mL) and Trichophyton rubrum (MIC₈₀ =0.25 μg/mL), as well as against Candida and Malassezia species. Unlike other antifungal agents, efinaconazole retains activity in the presence of keratin, indicating that more unbound drug is available at the site of action. Efinaconazole is efficacious in guinea-pig models of fungal infection. Efinaconazole is prepared by reaction of an epoxide intermediate with 4-methylenepiperidine.

Efinaconazole is a broad-spectrum triazole antifungal agent with activity against Acremonium, Aspergillus, Candida, Cryptococcus, Epidermophyton, Fusarium, Microsporum, Paecilomyces, Pseudallescheria, Scopulariopsis, Trichophyton, and Trichosporon. It inhibits the growth of T. rubrum and T. mentagrophytes clinical isolates with MIC values ranging from ≤2.0 to 60 ng/ml and of C. albicans isolates with MIC values ranging from ≤0.5 to >250 ng/ml. Efinaconazole inhibits sterol 14α-demethylase, which arrests ergosterol (Item No. 19850) biosynthesis at the fungal membrane.It inhibits ergosterol biosynthesis in T. mentagrophytes and C. albicans with IC₅₀ values of 7.0 and 0.40 ng/ml, respectfully. Topical formulations containing efinaconazole have been used for the treatment of onychomycosis.

Formal Name

αR-(2,4-difluorophenyl)-βR-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidineethanol

CAS Number

164650-44-6

Synonyms

• KP-103

Molecular Formula

C₁₈H₂₂F₂N₄O

Formula Weight

348.4

Purity

≥98%

Formulation

A crystalline solid

Solubility(Learn about Variance in Solubility)

• Chloroform: slightly soluble
• DMSO: >14 mg/ml
• Methanol: slightly soluble

λ_max

262 nm

SMILES

FC(C=C1F)=CC=C1[C@](CN2N=CN=C2)(O)[C@@H](C)N3CCC(CC3)=C

InChi Code

InChI=1S/C18H22F2N4O/c1-13-5-7-23(8-6-13)14(2)18(25,10-24-12-21-11-22-24)16-4-3-15(19)9-17(16)20/h3-4,9,11-12,14,25H,1,5-8,10H2,2H3/t14-,18-/m1/s1

InChi Key

NFEZZTICAUWDHU-RDTXWAMCSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room Temperature in continental US; may vary elsewhere

Stability

≥ 2 years