E17241 (Synonyms: 4-(1,3-Dithiolan-2-yl)-N-(3-hydroxypyridin-2-yl)benzamide) |
Catalog No.GC91933
One-Click Copy Product Info
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E17241 es un inductor de la expresión de ABCA1, el gen que codifica atp-transportador de cassette de Unión 1; Subfamilia A (ABCA1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1060968-92-4
Sample solution is provided at 25 µL, 10mM.
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E17241 is an inducer of the expression of ABCA1, the gene encoding ATP-binding cassette transporter 1; subfamily A (ABCA1).1 It induces the expression of ABCA1 in a reporter assay using HepG2 cells (EC50 = 280 nM). E17241 is also an agonist of peroxisome proliferator-activated receptors (PPARs).2 It induces PPAR-mediated gene expression in reporter assays using HepG2 cells expressing PPARγ, PPARα, or PPARδ (EC50s = 290, 3,900, and 879 nM, respectively). It increases the protein levels of ACBA1 in RAW 264.7 macrophages but not in the presence of siRNA targeting mRNA encoding PKCζ.1 E17241 (0.4, 2, or 10 ?M) increases cholesterol efflux in RAW 264.7 cells. It reduces plasma levels of cholesterol, alanine transaminase (ALT), and aspartate aminotransferase (AST) and hepatic levels of cholesterol and triglycerides, as well as decreases aortic lesion area, in an ApoE-/- mouse model of atherosclerosis when administered at a dose of 25 mg/kg. E17241 (50 mg/kg per day) decreases plasma glucose levels and body weight in KKAy diabetic mice fed a high-fat and high-glucose (HFHG) diet.2
References:
[1]. Xu, Y., Liu, C., Hang, X., et al.E17241 as a novel ABCA1 (ATP-binding cassette transporter A1) upregulator ameliorates atherosclerosis in miceArterioscler. Thromb. Vasc. Biol.41(6)e284-e298(2021).
[2]. Sheng, R., Li, Y., Wu, Y., et al.A pan-PPAR agonist E17241 ameliorates hyperglycemia and diabetic dyslipidemia in KKAy mice via up-regulating ABCA1 in islet, liver, and white adipose tissueBiomed. Pharmacother.172116200(2024).
| Cas No. | 1060968-92-4 | SDF | |
| Sinónimos | 4-(1,3-Dithiolan-2-yl)-N-(3-hydroxypyridin-2-yl)benzamide | ||
| Chemical Name | 4-(1,3-dithiolan-2-yl)-N-(3-hydroxypyridin-2-yl)benzamide | ||
| Canonical SMILES | OC1=CC=CN=C1NC(C(C=C2)=CC=C2C3SCCS3)=O | ||
| Formula | C15H14N2O2S2 | M.Wt | 318.4 |
| Solubility | DMSO: Soluble: ≥10 mg/ml | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1407 mL | 15.7035 mL | 31.407 mL |
| 5 mM | 628.1 μL | 3.1407 mL | 6.2814 mL |
| 10 mM | 314.1 μL | 1.5704 mL | 3.1407 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)