| CAS NO: | 50892-23-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 323.8 |
|---|---|
| Formula | C14H14ClN3O2S |
| CAS No. | 50892-23-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 65 mg/mL (200.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 65 mg/mL (200.7 mM) | |
| Other info | Chemical Name: [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-acetic acid InChi Key: SZRPDCCEHVWOJX-UHFFFAOYSA-N InChi Code: InChI=1S/C14H14ClN3O2S/c1-8-4-3-5-10(9(8)2)16-12-6-11(15)17-14(18-12)21-7-13(19)20/h3-6H,7H2,1-2H3,(H,19,20)(H,16,17,18) SMILES Code: O=C(O)CSC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1 |
| Synonyms | NSC 310038; NSC310038; WY-14643; WY 14643; NSC-310038; WY14643; Pirinixic Acid |
| In Vitro | In vitro activity: WY 14643 (10 μM) almost completely inhibits interleukin-1-induced production of interleukin-6 and prostaglandin and expression of cyclooxygenase-2 in aortic smooth-muscle cells, through repression of NF-κB signaling. WY14643 (250 μM) reduces VCAM-1 expression levels significantly, to 52 % of TNF-α-stimulated human endothelial cells. Pretreatment of endothelial cells with WY 14643 (10 μM) before TNF-α stimulation reduces U937 cell adhesion by 50%. Kinase Assay: Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively. Cell Assay: Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Pirinixic acid. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Pirinixic acid. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve |
|---|---|
| In Vivo | WY 14643 (1 mg/kg i.v. bolus) administration at 30 min before left anterior descending occlusion, causes significant reduction in infarct size of ~44% in rats subjected to regional myocardial ischemia (25 min) and reperfusion (2 h). WY 14643 (3 mg/kg) lowers basal plasma levels of glucose, triglycerides (-16% vs. untreated), and leptin (-52%), and also muscle triglyceride (-34%) and total long-chain acyl-CoAs (LCACoAs) (-41%) in high fat-fed rats. WY14643 substantially reduces visceral fat weight and total liver triglyceride content without increasing body weight gain. WY14643 enhances whole body insulin sensitivity (clamp glucose infusion rate increases 35% and glucose disposals 22%, vs. untreated). WY 14643 enhances insulin-mediated muscle glucose metabolic index (Rg') in red (47%) and white (63%) muscles as well as in white adipose tissue (90%), and reduces muscle triglyceride and LCACoA accumulation. |
| Animal model | Rats |
| Formulation & Dosage | 1 mg/kg i.v. bolus |
| References | Nature. 1990 Oct 18;347(6294):645-50; Nature. 1998 Jun 25;393(6687):790-3; FASEB J. 2002 Jul;16(9):1027-40. |
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