ChemicalBook > CAS DataBase List > PF-06282999

PF-06282999

Product Name: PF-06282999
CAS No.: 1435467-37-0
Chemical Name: PF-06282999
Synonyms: CS-2543;PF-06282999;PF-06282999 (Free base);PF-06282999 (PF06282999;PF-06282999 >=98% (HPLC);PF-06282999, 10 mM in DMSO;PF-06282999;PF 06282999;PF06282999;PF06282999,Glutathione Peroxidase,PF 06282999,PF-06282999,Inhibitor,inhibit;1(2H)-Pyrimidineacetamide, 6-(5-chloro-2-methoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-;2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide
CBNumber: CB93145903
Molecular Formula: C13H12ClN3O3S
Formula Weight: 325.77
MOL File: 1435467-37-0.mol

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PF-06282999 Property

Density: 1.52±0.1 g/cm3(Predicted)
storage temp.: room temp
solubility: DMSO:30.0(Max Conc. mg/mL);92.1(Max Conc. mM)
form: powder
pka: 6.85±0.40(Predicted)
color: white to beige

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0375
Product name: PF-06282999
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $89.3
Updated: 2025/07/31

Cayman Chemical

Product number: 28406
Product name: PF-06282999
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 28406
Product name: PF-06282999
Packaging: 5mg
Price: $97
Updated: 2024/03/01

Cayman Chemical

Product number: 28406
Product name: PF-06282999
Packaging: 10mg
Price: $172
Updated: 2024/03/01

Cayman Chemical

Product number: 28406
Product name: PF-06282999
Packaging: 25mg
Price: $374
Updated: 2024/03/01

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PF-06282999 Chemical Properties,Usage,Production

Uses

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

Biological Activity

PF-06282999 is an orally active thiouracil class myeloperoxidase (MPO) suicide substrate (kinact/KI = 11600 M-1s-1) th at targets MPO heme group for mechanism-based irreversible inactivation wtih high selectivity over thyroid peroxidase (TPO kinact/KI <3 M-1s-1) and heme-containing cytochrome P450 (CYP) isoforms (IC50 >100 μM). PF-06282999 effectively inhibits MPO activity in human blood stimulated by LPS ex vivo (IC50 = 1.9 μM) and in blood of LPS-treated cynomolgus monkeys in vivo (5-80 mg/kg p.o. 1hr post LPS i.v.) with good pharmacokinetics and oral availability (100%/86%/75%/76% in mice/rats/dogs/monkeys). PF-06282999 also exhibits weak PXR activating activity (EC50/Emax = 279 μM/9.36-fold vs.0.8 μM/19.6-fold with rifampin).

in vivo

PF-06282999 is moderately bound to plasma proteins across preclinical species and humans. The blood/plasma ratios for PF-06282999 are 1.1, 1.1, 0.91, 1.2, and 0.94 in mice, rats, dogs, monkeys, and humans, respectively, suggesting that PF-06282999 is equally distributed into plasma and red blood cells^[1]. The in vivo pharmacokinetics of PF-06282999 are examined in greater detail in mice, rats, dogs, and monkeys, wherein it is demonstrated to have low CLp in mice (10.1 mL/min/kg), dogs (3.39 mL/min/kg), monkeys (10.3 mL/min/kg) and moderate CLp in rats (41.8 mL/min/kg). The terminal plasma elimination half-lives (t1/2) range from 0.75 to 3.3 h in the four species. Approximately 26-32% of the iv dose of PF-06282999 is excreted in the unchanged form in rat, dog, and monkey urine, wherein it is also shown that it is well distributed with steady state distribution volumes (Vdss) ranging from 0.5-2.1 L/kg in mice, rats, dogs, and monkeys. Following oral administration, PF-06282999 is rapidly (Tmax=0.78-1.70 h) and well absorbed in mice, rats, dogs, and monkeys with oral bioavailability values of 100%, 86%, 75%, and 76%, respectively^[2].

References

[1] Dong JQ, et al. Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans. Drug Metab Dispos. 2016 Feb;44(2):209-19. DOI:10.1124/dmd.115.067868
[2] Ruggeri RB, et al. Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. J Med Chem. 20 DOI:10.1021/acs.jmedchem.5b00963

PF-06282999 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PF-06282999 manufacturers

Career Henan Chemical Co

Product: PF-06282999 1435467-37-0
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 20kg
Release date: 2019-12-23

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PF-06282999

PF-06282999 (Free base)

2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide

CS-2543

PF-06282999;PF 06282999;PF06282999

1(2H)-Pyrimidineacetamide, 6-(5-chloro-2-methoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-

PF-06282999 >=98% (HPLC)

PF06282999,Glutathione Peroxidase,PF 06282999,PF-06282999,Inhibitor,inhibit

PF-06282999, 10 mM in DMSO

PF-06282999 (PF06282999

1435467-37-0