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| 10mg |
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| 50mg |
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| 250mg |
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Purity: ≥98%
Pirinixic Acid (also known as NSC 310038; NSC310038; WY-14643; WY 14643) is a novel, highly potent and selective peroxisome proliferator and activator of PPARα with important biological activity. It inhibits PPARα with an EC50 of 1.5 μM. Pirinixic Acid was under development for preventing severe cardiac dysfunction, cardiomyopathy and heart failure as a result of lipid accumulation within cardiac myocytes.
| ln Vitro |
As an agonist of PPARα, pirinixic acid (Wy-14643) has EC50s of 0.63 μM and 32 μM for PPARα and PPARγ in mice, and 5.0 μM, 60 μM, 35 μM, and PPARδ for PPARα and PPARγ in humans [1]. In synovial fibroblasts, pirinixic acid (Wy-14643; 0, 10, 100 μM) increases the expression of the PPAR-α protein. LPS-stimulated synovial fibroblasts' generation of NO and PGE2 is inhibited by pirinixic acid (0, 10, 100 μM). Additionally, pirinixic acid efficiently inhibits LPS-induced NF-kB activation, IkB phosphorylation, and TF in synovial fibroblasts as well as downregulating the production of inflammatory mediators in these cells, including VCAM-1, ICAM-1, ET-1, and TF. PPAR-α silenced cells, whereas pirinixic acid had little effect on NF-kB nuclear translocation [2].
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| ln Vivo |
In obese rats, pirinixic acid (Wy-14643; 10 mg/kg, IV) lowers MDA levels and liver damage. In the Sham and ischemia-reperfusion (IR) groups, pirinixic acid likewise increased SIRT1 activity, but it had no effect on the production of SIRT3 protein. In rats, pirinixic acid can prevent endoplasmic reticulum stress (ERS) and raise NAD+ and ATP levels [3].
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| Animal Protocol |
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| References |
[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[2]. Huang D, et al. PPAR-α Agonist WY-14643 Inhibits LPS-Induced Inflammation in Synovial Fibroblasts via NF-kB Pathway. J Mol Neurosci. 2016 Aug;59(4):544-53. [3]. Pantazi E, et al. PPARα Agonist WY-14643 Induces SIRT1 Activity in Rat Fatty Liver Ischemia-Reperfusion Injury. Biomed Res Int. 2015;2015:894679 |
| Molecular Formula |
C14H14CLN3O2S
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| Molecular Weight |
323.8
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| CAS # |
50892-23-4
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| Related CAS # |
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| SMILES |
ClC1C([H])=C(N=C(N=1)SC([H])([H])C(=O)O[H])N([H])C1=C([H])C([H])=C([H])C(C([H])([H])[H])=C1C([H])([H])[H]
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| InChi Key |
SZRPDCCEHVWOJX-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-acetic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0883 mL | 15.4416 mL | 30.8833 mL | |
| 5 mM | 0.6177 mL | 3.0883 mL | 6.1767 mL | |
| 10 mM | 0.3088 mL | 1.5442 mL | 3.0883 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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