Posaconazole

Posaconazole Properties

Melting point	170-1720C
Boiling point	850.7±75.0 °C(Predicted)
Density	1.36±0.1 g/cm3(Predicted)
Flash point	9℃
storage temp.	-20°C
solubility	Chloroform (Slightly), Methanol (Slightly)
pka	14.72±0.20(Predicted)
form	powder
color	white to beige
optical activity	[α]/D -24 to -32°, c = 1.0 in chloroform-d
Merck	14,7602
InChIKey	RAGOYPUPXAKGKH-XAKZXMRKSA-N
SMILES	[C@]1(OC[C@@H](COC2C=CC(N3CCN(C4=CC=C(N5C=NN([C@@H](CC)[C@@H](O)C)C5=O)C=C4)CC3)=CC=2)C1)(CN1N=CN=C1)C1=CC=C(F)C=C1F \|&1:0,3,22,25,r\|
CAS DataBase Reference	171228-49-2(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS02,GHS06,GHS08

Signal word

Danger

Hazard statements

H225-H301+H311+H331-H370

Precautionary statements

P210-P260-P280-P301+P310-P311

Hazard Codes

F,T

Risk Statements

11-23/24/25-39/23/24/25

Safety Statements

7-16-36/37-45

RIDADR

UN1230 - class 3 - PG 2 - Methanol, solution

WGK Germany

3

RTECS

XZ5481020

HS Code

3204.90.0000

NFPA 704

	0
2		0

Posaconazole price More Price(6)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Sigma-Aldrich(India)	SML2287	Posaconazole ≥98% (HPLC)	171228-49-2	5MG	₹13390.53	2022-06-14	Buy
Sigma-Aldrich(India)	SML2287	Posaconazole ≥98% (HPLC)	171228-49-2	25MG	₹53854.38	2022-06-14	Buy
Sigma-Aldrich(India)	P-103	Posaconazole solution 2.0?mg/mL in methanol, ampule of 1?mL, certified reference material, Cerilliant?	171228-49-2	1ML	₹16425.5	2022-06-14	Buy
Sigma-Aldrich(India)	32103	Posaconazole VETRANAL?, analytical standard	171228-49-2	25MG	₹11236.35	2022-06-14	Buy
TCI Chemicals (India)	P2477	Posaconazole	171228-49-2	10MG	₹3600	2022-05-26	Buy

Product number	Packaging	Price	Buy
SML2287	5MG	₹13390.53	Buy
SML2287	25MG	₹53854.38	Buy
P-103	1ML	₹16425.5	Buy
32103	25MG	₹11236.35	Buy
P2477	10MG	₹3600	Buy

Posaconazole Chemical Properties,Uses,Production

Description

Posaconazole, launched in the UK, is the newest member of the azole class of antifungal agents to reach the market. It is indicated for the treatment and prophylaxis of a range of invasive fungal infections, including aspergillosis,fusariosis, chromoblastomycosis, mycetoma, and coccidiomycosis in patients who are refractory to, or intolerant of, standard therapy with amphotericin B and/or itraconazole. In the US, it is approved for the prophylaxis of invasive Aspergillus and Candida infections in patients 13 years of age who are at high risk of developing these infections due to being severely immunocompromised. Additionally, it is approved for the treatment of oropharyngeal candidiasis. Posaconazole has an expanded spectrum of activity over other members of the azole antifungals. In addition to potent activity against refractory cases of aspergillosis and fluconazole-resistant Candida, it demonstrates activity against Zygomycetes.

Chemical Properties

White Solid

Uses

Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM

Definition

ChEBI: An N-arylpiperazine that consists of piperazine carrying two 4-substituted phenyl groups at positions 1 and 4. A triazole antifungal drug.

Antimicrobial activity

The spectrum includes dimorphic fungi (Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Pen. marneffei, and Spor. schenckii), molds (Aspergillus spp., Mucor spp., Rhizomucor spp. and Rhizopus spp.), some dematiaceous fungi and yeasts (Candida spp. and Cryptococcus spp.).

General Description

Technetium (^99mTc) exametazime is a mixture of unstablelipophilic enantiomers that rapidly cross the blood-brain barrierand is trapped in the tissues. The proposed trapping mechanismfor localization includes reduction by glutathione. Asimilar diffusion and trapping process occurs with autologouslymphocytes in vitro.
Exametazime is also known as hexamethylpropyleneamineoxime or HMPAO. The radiolabeled complex is indicated for cerebral perfusion in stroke, but is most commonlyused for the radiolabeling of autologous leukocytesas an adjunct in the localization of intra-abdominal infectionand inflammatory bowel disease.
Each kit includes several components: (a) reaction vialscontaining a mixture of exametazime, stannous chloride,and sodium chloride; (b) vials of 1% methylene blue; (c)vials of phosphate buffer in 0.9% NaCl; and (d) 0.45-μm syringefilters. Product preparation depends on the intendeduse.

Pharmaceutical Applications

A synthetic triazole available for oral administration.

Pharmacokinetics

C_max 200 mg oral: 0.5 mg/L after 4 h
Plasma half-life: 35 h
Volume of distribution: 1774 L
Plasma protein binding: >98%
Absorption
Oral absorption is slow. Absorption from the gastrointestinal tract is improved if the drug is given with a high-fat meal. Blood concentrations increase in proportion to dosage up to 800 mg.
Distribution
It is extensively distributed into body tissues.
Metabolism and excretion
It is not as extensively metabolized by the hepatic cytochrome P₄₅₀ system as other triazole antifungals. More than 70% of an administered dose is eliminated in the feces, predominantly as unchanged drug. The remainder is excreted as glucuronidated derivatives in the urine. Posaconazole is a substrate for intestinal P-glycoprotein,an adenosine triphosphate-dependent plasma membrane transporter responsible for drug efflux from cells. Multiple peaks in blood concentrations have been observed, suggesting that effluxed drug is reabsorbed into the systemic circulation.

Clinical Use

Invasive aspergillosis
Fusarium infection
Chromoblastomycosis and mycetoma
Coccidioidomycosis
Oropharyngeal candidosis
Prophylaxis of invasive fungal infections in patients at serious risk
With the exception of oropharyngeal candidosis and prophylaxis, use is presently restricted to patients with disease that is refractory to other antifungal drugs, or who are intolerant to them.

Side effects

It is generally well tolerated even for long periods. Unwanted effects include gastrointestinal discomfort and mild to moderate, transient abnormalities of liver enzymes. Rare side effects include cholestasis and hepatic failure.

Posaconazole Preparation Products And Raw materials

Raw materials

O-Benzyl Posaconazole

Preparation Products

Posaconazole Suppliers

Global( 708)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
Dr. Reddy's Laboratories Ltd	+91-4049002900 +91-4049002900	Hyderabad, India	165	58	Inquiry
SGMR PHARMACEUTICALS PVT LTD	+91-9032001889 +91-9032001889	Telangana, India	83	58	Inquiry
SEUTIC	+91-8309787199 +91-8309787199	Hyderabad, India	124	58	Inquiry
Prajna generics pvt ltd	+91-9441174873 +91-9441174873	Hyderabad, India	24	58	Inquiry
Metrochem API Private Limited	+91-4069069999 +91-4069069999	Telangana, India	78	58	Inquiry
Apotex Pharmachem India Pvt Ltd	+91-8022891034 +91-8022891000	Karnataka, India	109	58	Inquiry
Honour Lab Limited	+919845977466	Telangana, India	164	58	Inquiry
Hetero Drugs Limited	+91-4023704923 +91-4023704923	Telangana, India	296	58	Inquiry
Bajaj Healthcare Ltd	+91-2266177400 +91-2266177400	Maharashtra, India	86	58	Inquiry
Om Pharmaceutical Industries	+91-2502344639 +91-9822376539	Maharashtra, India	32	58	Inquiry

Supplier	Advantage
Dr. Reddy's Laboratories Ltd	58
SGMR PHARMACEUTICALS PVT LTD	58
SEUTIC	58
Prajna generics pvt ltd	58
Metrochem API Private Limited	58
Apotex Pharmachem India Pvt Ltd	58
Honour Lab Limited	58
Hetero Drugs Limited	58
Bajaj Healthcare Ltd	58
Om Pharmaceutical Industries	58

Posaconazole Spectrum

Posaconazole(171228-49-2)¹HNMR

171228-49-2(Posaconazole)Related Search:

Ketoconazole Miconazole nitrate Dichloromethylphenylsilane Fluconazole Itraconazole

Triphenylphosphine Methyltriphenylphosphonium bromide 2-Phenylphenol SAPERCONAZOLE 5-Methyl-1H-benzotriazole

1-(4-Aminophenyl)-4-(4-hydroxyphenyl)piperazine 2-[(1S,2S)-1-ethyl-2-bezyloxypropyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]- 3H-1,2,4-Triazol-3-one, (5R-cis)-Toluene-4-sulfonic acid 5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-yl)methyltetrahydrofuran-3-ylmethyl ester Ravuconazole 1,3-PROPANEDIOL, 2-[2-(2,4-DIFLUOROPHENYL)-2-PROPEN-1-YL]-

(S)-4-(2,4-difluorophenyl)-2-(hydroxymethyl)pent-4-en-1-ylisobutyrate 1-((2S,3R)-2-(benzyloxy)pentan-3-yl)-N-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)hydrazine-1-carboxamide PHENYL {4-[4-(4-HYDROXYPHENYL)PIPERAZIN-1-YL]PHENYL}CARBAMATE

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4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one Posaconazole(Form Ⅲ) Posaconazole 2,5-Anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl]phenyl]-1-piperazinyl]phenoxy]methyl]-1-(1H-1,2,4-triazol-1-yl)-D-threo-pentitol Sch 56592 HYDROXYPROPYL]-2,4-DIHYDRO-3H-1,2,4-TRIAZOL-3-ONE Posaconazole for research 1-((1S,2S)-1-Ethyl-2-hydroxypropyl)-4-{4-[4-(4-{[(5S,3R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazolylmethyl)oxolan-3-yl]methoxy}phenyl)piperazinyl]phenyl}-1,2,4-triazolin-5-one Aids058495 Aids-058495 4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one POSACONAZOLE whatsapp Posconazole 4-(4-(4-(4-(((3R,5R)-5-(3,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-yl)tetrahydrofuran-3-yl)Methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one 4-{4-[4-(4-{[(3S,5R)-5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-ylMethyl)oxolan-3-yl]Methoxy}phenyl)piperazin-1-yl]phenyl}-1-[(2S,3S)-2-hydroxypentan-3-yl]-4,5-dihydro-1H-1,2,4-triazol-5-one 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)Methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)Methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one D-threo-Pentitol,2,5-anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl]phenyl]-1-piperazinyl]phenoxy]Methyl]-1-(1H-1,2,4-triazol-1-yl)- 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)-tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-2H-1,2,4-triazol-3(4H)-one Posaconazole 4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one Posaconazole solution Posaconazole Amorphous Posaconazole, >=99% Technetium (99mTc) exametazime EOS-60773 POSACONAZOLE(FORM Ⅰ) Posaconazole and intermediates posaconazote Posacozole CS-140 PO-CI CIII Posaconazole - SCH 56592 | Noxafil Posaconazole USP/EP/BP Posaconazole(amorphous & Form Ⅰ& Form III) 2,5-Anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl US-DMF No.: 028314 US-DMF No.: 030886 US-DMF No.:032346 PosaconazoleQ: What is Posaconazole Q: What is the CAS Number of Posaconazole Q: What is the storage condition of Posaconazole Q: What are the applications of Posaconazole 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorobenzyl)tetrahydrofuran-3 Noxafil Pcz Pos Pasaconazole Posaconazole D3 Bosaconazole Poconazole Posaconazole（RRSS） Posaconazole(amorphous & Form Ⅰ& Form III) Schering 56592 Schering-56592 Posaconazole Diastereoisomer Related Compod 3 171228-49-2 71228-49-2 133712-26-1 17122-49-2 C37H42F2N8O4 API Noxafil