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Fosfluconazole

Product Name
Fosfluconazole
CAS No.
194798-83-9
Chemical Name
Fosfluconazole
Synonyms
Prodif;CS-969;Fosfluconazol;Fosfluconazole(INN);Fosfluconazole, >=98%;Dihydrogen phosphate ester;Fungal,Inhibitor,Fosfluconazole,inhibit;2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propyl dihydrogen phosphate;PHARMA PRODUCT FLUCONAZOLE USP 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1,2,4-TRIAZOL-1-YL) PROPAN-2-OL;2-(2,4-Difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-yl dihydrogen phosphate (Efinaconazole?Impurity)
CBNumber
CB71120322
Molecular Formula
C13H13F2N6O4P
Formula Weight
386.25
MOL File
194798-83-9.mol
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Fosfluconazole Property

Melting point:
223-224°
Boiling point:
701.5±70.0 °C(Predicted)
Density 
1.70±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 6.2 mg/mL (16.05 mM)
form 
Solid
pka
1.44±0.10(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6032
Product name
Fosfluconazole
Purity
98.08%
Packaging
10mg
Price
$60
Updated
2021/12/16
ChemScene
Product number
CS-6032
Product name
Fosfluconazole
Purity
98.08%
Packaging
25mg
Price
$120
Updated
2021/12/16
ChemScene
Product number
CS-6032
Product name
Fosfluconazole
Purity
98.08%
Packaging
50mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-6032
Product name
Fosfluconazole
Purity
98.08%
Packaging
100mg
Price
$288
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0002762
Product name
FOSFLUCONAZOLE
Purity
95.00%
Packaging
100MG
Price
$2317.35
Updated
2021/12/16
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Fosfluconazole Chemical Properties,Usage,Production

Description

Fosfluconazole is a phosphate prodrug of fluconazole, and it was launched in Japan as an intravenous injection for the treatment of candidiasis and cryptococcosis infections. Fluconazole, a triazole antifungal agent, is a selective inhibitor of fungal cytochrome P450 sterol C-14 alpha-demethylation, and it is widely used for the treatment of patients with serious systemic fungal infections. Fluconazole is marketed in both oral and intravenous formulations, the latter being a dilute (2 mg/ mL) infusion in saline due to the relatively poor water solubility of the drug. In patients needing high doses (>400 mg) of fluconazole, a drawback of the IV formulation is the requirement of a high-volume infusion, which is undesirable in critically ill patients in whom fluid overload must be avoided. Fosfluconazole is a prodrug with approximately 40-fold higher water solubility than fluconazole, thereby achieving a substantial reduction in infusion volume. It is prepared in three steps starting from fluconazole. In the first step, fluconazole is converted to its dibenzyl phosphite derivative by reaction with phosphorous trichloride and benzyl alcohol. Subsequent oxidation of the phosphite to the corresponding phosphate with hydrogen peroxide and cleavage of the benzyl protecting groups by hydrogenolysis affords fosfluconazole. In vitro, fosfluconazole is at least 25-fold less potent than fluconazole against single isolates of Candida species and Cryptococcus neoformans. In vivo, it is rapidly hydrolyzed to fluconazole by phosphatase enzymes and exhibits similar efficacy to fluconazole in experimental models of fungal disease. The hydrolysis potential of fosfluconazole was initially demonstrated in homogenates of kidney, lung and liver of rat, dog, and human. Subsequently, in clinical trials with healthy volunteers (n=24), fosfluconazole was shown to hydrolyze rapidly and almost completely to provide a 97% mean bioavailability of fluconazole. Less than 1% of the administered dose of fosfluconazole was excreted unchanged in the urine, with the majority (85.6%) of the dose eliminated as fluconazole. The terminal half-life was about 2.3 hours, and the volume of distribution was 0.2 L/kg. The time to reach steady state drug levels with 500 mg daily dose was about 10 days, which could be shortened to 3 days by administering loading doses of 1000 mgs on days 1 and 2 followed by 500 mg daily. Further studies showed that hepatic or renal impairment did not significantly alter the pharmacokinetic profile of fosfluconazole. In phase III studies in patients with deep-seated mycosis due to Candida or Cryptococcus (n=160), a 2-day loading dose regimen of fosfluconazole provided efficacy range of 73.8% (in Japanese patients) to 91.7% (patients of non-Japanese origin). The adverse events seen in these trials were similar to those previously known with fluconazole therapy and included rash (3.1%), abnormal liver function values (2.5%), asthma (1.9%), and lightheadedness (1.9%).

Originator

Pfizer (Japan)

Definition

ChEBI: Fosfluconazole is a member of triazoles, a triazole antifungal drug and a conazole antifungal drug. It has a role as a prodrug. It is functionally related to a fluconazole.

brand name

Prodif

Fosfluconazole Preparation Products And Raw materials

Raw materials

Preparation Products

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Fosfluconazole Suppliers

AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38631
Advantage
58
Abblis Chemicals LLC
Tel
--
Fax
--
Email
info@abblis.com
Country
United States
ProdList
1272
Advantage
0
MedChemExpress
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58
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View Lastest Price from Fosfluconazole manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Fosfluconazole 194798-83-9
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-10-11
Career Henan Chemical Co
Product
Fosfluconazole 194798-83-9
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

194798-83-9, FosfluconazoleRelated Search:


  • 2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propyl dihydrogen phosphate
  • Prodif
  • Fosfluconazole, >=98%
  • PHARMA PRODUCT FLUCONAZOLE USP 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1,2,4-TRIAZOL-1-YL) PROPAN-2-OL
  • Dihydrogen phosphate ester
  • CS-969
  • Fosfluconazole(INN)
  • 1H-1,2,4-Triazole-1-ethanol, α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-ylmethyl)-, 1-(dihydrogen phosphate)
  • 1H-1,2,4-Triazole-1-ethanol, a-(2,4-difluorophenyl)-a-(1H-1,2,4-triazol-1-ylmethyl)-,1-(dihydrogen phosphate)
  • Fungal,Inhibitor,Fosfluconazole,inhibit
  • 2-(2,4-Difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-yl dihydrogen phosphate (Efinaconazole?Impurity)
  • Fosfluconazol
  • 194798-83-9
  • C13H13F2N6O4P
  • Amines
  • API
  • Chiral Reagents
  • Heterocycles