JY-2
Based on 3 publication(s) in Google Scholar
JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.75%
- CAS 番号: 339103-05-8
- 分子式: C13H7Cl2N3O
- 分子量:292.12
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 JY-2
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生物活性
製品説明
IC50 & Target
22 μM (FoxO1 transcriptional activity)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.7 μM
Compound: 7f
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Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
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[PMID: 23046966] |
体外実験
JY-2 (10-100 μM; 24 h) reduces palmitic acid (PA; HY-N0830)-induced lipotoxicity in HepG2 and INS-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and INS-1 cells
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Concentration:10, 50 and 100 μM
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Incubation Time:24 h
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Result:Reduced palmitic acid (PA)-induced G6Pase and PEPCK mRNA expression. Inhibited PA-induced lipid accumulation. Reduced PA-induced mRNA expression of ER stress markers (ATF3, CHOP and GRP78).
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Cell Line:HepG2 cells
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Concentration:10, 50 and 100 μM
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Incubation Time:4 h; in the presence of PA (500μM)
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Result:Increased p-FoxO1 levels in the whole cell lysate with a concurrent reduction in nuclear FoxO1 levels.
体内実験
Pharmacokinetic parameters of JY-2[1]
| Parameters | i.v. (20 mg/kg) | p.o. (50 mg/kg) |
| AUCall (ng·h/mL) | 5017 ± 1038 | 12270 ± 2775 |
| AUCinf.obs (ng·h/mL) | 5030 ± 1037 | 12400 ± 2753 |
| Cmax (ng/mL) | 10790 ± 3269 | 6826 ± 2342 |
| Tmax (h) | 0.1 ± 0.1 | 0.8 ± 0.7 |
| T1/2 (h) | 0.8 ± 0.2 | 1.3 ± 0.4 |
| MRTinf.obs (h) | 0.7 ± 0.1 | 2.0 ± 0.1 |
| F (%) | 97.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice[1]
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Dosage:50, 100, 200 mg/kg
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Administration:Oral, three times for two days (9:00 AM, 7:00 PM, 9:00 AM on the next day)
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Result:Improved glucose tolerance. Significantly reduced the expression of G6Pase and PEPCK mRNA in the liver. Enhanced mRNA expression of insulin and PDX-1 in the pancreas.
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Animal Model:db/db mice and C57BL/6J mice, high fat-diet-induced obese diabetic (DIO) model[1]
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Dosage:50, 100 mg/kg
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Administration:Oral, once daily for 4 weeks
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Result:Decreased the levels of fasting blood glucose, improved glucose tolerance. The expression of ColIV, a fibrosis marker, was also lowered.
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Animal Model:C57BL/6J mice[1]
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Dosage:20 mg/kg or 50 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Showed an overall good pharmacokinetic profile.
化学情報
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CAS 番号 339103-05-8
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性状 Solid
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分子量 292.12
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分子式 C13H7Cl2N3O
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Color White to off-white
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SMILES
ClC1=CC(Cl)=C(C2=NC(C3=CC=CC=N3)=NO2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer. [Abstract]2024 Sep 10;15(9):662. PMID: 39256356 -
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Int J Chron Obstruct Pulmon Dis
Azithromycin Mitigates Tobacco Smoke-Induced Lung Senescence by Modulating the FOXO3A/CCND1 Signaling Pathway. [Abstract]2025 Nov 11:20:3631-3645. PMID: 41244262
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (342.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4233 mL | 17.1163 mL | 34.2325 mL | 85.5813 mL |
| 5 mM | 0.6847 mL | 3.4233 mL | 6.8465 mL | 17.1163 mL | |
| 10 mM | 0.3423 mL | 1.7116 mL | 3.4233 mL | 8.5581 mL | |
| 15 mM | 0.2282 mL | 1.1411 mL | 2.2822 mL | 5.7054 mL | |
| 20 mM | 0.1712 mL | 0.8558 mL | 1.7116 mL | 4.2791 mL | |
| 25 mM | 0.1369 mL | 0.6847 mL | 1.3693 mL | 3.4233 mL | |
| 30 mM | 0.1141 mL | 0.5705 mL | 1.1411 mL | 2.8527 mL | |
| 40 mM | 0.0856 mL | 0.4279 mL | 0.8558 mL | 2.1395 mL | |
| 50 mM | 0.0685 mL | 0.3423 mL | 0.6847 mL | 1.7116 mL | |
| 60 mM | 0.0571 mL | 0.2853 mL | 0.5705 mL | 1.4264 mL | |
| 80 mM | 0.0428 mL | 0.2140 mL | 0.4279 mL | 1.0698 mL | |
| 100 mM | 0.0342 mL | 0.1712 mL | 0.3423 mL | 0.8558 mL |
JY-2 関連分類
HY-153347 関連分類
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