- PF-06282999
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- $1.00 / 1g
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2019-12-24
- CAS:1435467-37-0
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 20kg
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| | PF-06282999 Basic information |
| Product Name: | PF-06282999 | | Synonyms: | 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 | | CAS: | 1435467-37-0 | | MF: | C13H12ClN3O3S | | MW: | 325.77 | | EINECS: | | | Product Categories: | | | Mol File: | 1435467-37-0.mol |  |
| | PF-06282999 Chemical Properties |
| 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 |
| | PF-06282999 Usage And Synthesis |
| 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). |
| | PF-06282999 Preparation Products And Raw materials |
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