Rivoglitazone
Based on 1 Customer Validation
Rivoglitazone (R-106056) is an orally active, selective PPARγ agonist with an EC50 of 0.22 μM for hPPARγ. Rivoglitazone regulates fatty acid storage and uptake, glucose homeostasis, and cardiac glucose/fatty acid metabolism. Rivoglitazone reduces levels of hyperglycemia, hyperinsulinemia, and hypertriglyceridemia, decreases hepatic glucose production, and accelerates plasma triglyceride clearance. Rivoglitazone induces a reduction in glycated hemoglobin A1C, while causing peripheral edema and weight gain. Rivoglitazone can be used in research related to type 2 diabetes.
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: 98.59%
- CAS 番号: 185428-18-6
- 分子式: C20H19N3O4S
- 分子量:397.45
-
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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Anti-diabetic Compound Library
HY-L040
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Orally Active Compound Library
HY-L061
-
Anti-Obesity Compound Library
HY-L087
-
Transcription Factor-Targeted Library
HY-L090
-
Lipid Metabolism Compound Library
HY-L091
-
Antidepressant Compound Library
HY-L108
-
Human Metabolite Library
HY-L123
-
Nuclear Receptor Compound Library
HY-L126
-
Osteogenesis Compound Library
HY-L131
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Mitochondrial Protection Compound Library
HY-L144
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Activators Library
HY-L159
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Aging Compound Library
HY-L034
生物活性
|
PPARγ 0.22 μM (EC50) |
Rivoglitazone exhibits higher potency in activating PPAR-γ compared with Pioglitazone (HY-13956) and Rosiglitazone (HY-17386), with 16.4-fold and 3.6-fold increases, respectively[1].
Rivoglitazone (0.001-10 μM; 24 h) potently and selectively activates hPPARγ in HT-1080 cells with an EC50 of 0.22 μM, while it exhibits only extremely weak activity against hPPARα and no activity against hPPARδ[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-t | AUC0-inf | CLtotal | Vss | T1/2 |
|---|---|---|---|---|---|---|---|
| Rat[4] | 0.1, 0.5 mg/kg | i.v. | 4.53 (0.1 mg/kg) μg·h/mL | 4.67 (0.1 mg/kg) μg·h/mL | 0.329 (0.1 mg/kg) mL/min/kg | 0.125 (0.1 mg/kg) L/kg | 4.55 (0.1 mg/kg) h |
Rivoglitazone (0.03-1 mg/kg; p.o.; daily; 14 days) exerts potent dose-dependent glucose-lowering (ED50 0.47 mg/kg) and adiponectin-increasing effects in male db/db mice[3].
Rivoglitazone (0.1 mg/kg; p.o.; daily; 7-8 days) improves whole-body insulin resistance, as shown by a 40% increase in steady-state GIR, and lowers plasma TG primarily by accelerating TG elimination in male ZF rats[3].
Rivoglitazone (0.0986-1 mg/kg; i.v., saphenous vein; p.o., nasal tubing) exhibits low clearance, low volume of distribution, high oral bioavailability (≥76.1%), and dose-proportional exposure in male cynomolgus monkeys, with O-demethylation as the main metabolic pathway and balanced excretion in urine and feces[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BKS.Cg-it +Lepr^db/+Lepr^db/Jcl (male, 8 weeks old)[3]
-
Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
-
Administration:p.o.; daily; 14 days
-
Result:Decreased plasma glucose levels in a dose-dependent manner, with an ED50 of 0.47 mg/kg compared to pioglitazone (70 mg/kg).
Strikingly increased plasma adiponectin levels in a dose-dependent manner, reaching 40 μg/mL at 1 mg/kg.
-
Animal Model:Crlj:ZUC-Leprfa (male, 9 weeks old)[3]
-
Dosage:0.1 mg/kg
-
Administration:p.o.; daily; 7-8 days
-
Result:Significantly increased the steady-state glucose infusion rate (GIR) to 36.6 mg·kg-1·min-1 (vs. control 26.0 mg·kg-1·min-1) and decreased steady-state plasma insulin to 28.5 ng/mL (vs. control 31.7 ng/mL).
Reduced basal plasma TG to 227 mg/dL, decreased the area under the TG curve (AUCTG) after lipid load to 939 h·mg/dL, and increased the TG elimination rate constant to 0.0689 min-1, with no effect on TG production rate.
化学情報
-
CAS 番号 185428-18-6
-
性状 Solid
-
分子量 397.45
-
分子式 C20H19N3O4S
-
Color White to off-white
-
SMILES
O=C(N1)SC(CC2=CC=C(OCC3=NC4=CC=C(OC)C=C4N3C)C=C2)C1=O
-
別名
R-106056
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 10 mg/mL (25.16 mM; ultrasonic and warming and heat to 80°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
-
データシート (275 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Koffarnus RL, et al. Rivoglitazone: a new thiazolidinedione for the treatment of type 2 diabetes mellitus. Ann Pharmacother. 2013;47(6):877-885. [Content Brief]
[2]. Pfanzagl B, et al. The Transient Receptor Potential Vanilloid 4 Agonist RN-1747 Inhibits the Calcium Response to Histamine. Pharmacology. 2019;104(3-4):166-172. [Content Brief]
[3]. Kanda S, et al. Potent antidiabetic effects of rivoglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, in obese diabetic rodent models. J Pharmacol Sci. 2009;111(2):155-166. [Content Brief]
[4]. Uchiyama M, et al. Pharmacokinetics, metabolism, and disposition of rivoglitazone, a novel peroxisome proliferator-activated receptor γ agonist, in rats and monkeys. Drug Metab Dispos. 2011;39(4):653-666. [Content Brief]
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 | 2.5160 mL | 12.5802 mL | 25.1604 mL | 62.9010 mL |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0321 mL | 12.5802 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 mL | 6.2901 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6774 mL | 4.1934 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1450 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0064 mL | 2.5160 mL |
Rivoglitazone 関連分類
HY-106181 関連分類
Powered by Bioz