2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. Rivoglitazone

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.

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Rivoglitazone

Rivoglitazone Chemical Structure

CAS No. : 185428-18-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Rivoglitazone:

Rivoglitazone Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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Description

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[1][2][3][4].

IC50 & Target[3]

PPARγ

0.22 μM (EC50)

In Vitro

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.

Rivoglitazone Related Antibodies
Parmacokinetics
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
In Vivo

Rivoglitazone (0.03-1 mg/kg; p.o.; daily; 14-15 days) exerts potent dose-dependent glucose-lowering (ED50 0.19-0.20 mg/kg) and TG-lowering (ED50 0.21-0.22 mg/kg) effects, increases pancreatic insulin content, modulates hepatic and cardiac gene expression to reduce gluconeogenesis and shift cardiac metabolism toward glucose utilization in male ZDF rats[3].
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.
Molecular Weight

397.45

Formula

C20H19N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1)SC(CC2=CC=C(OCC3=NC4=CC=C(OC)C=C4N3C)C=C2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5160 mL 12.5802 mL 25.1604 mL
5 mM 0.5032 mL 2.5160 mL 5.0321 mL
View the 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.

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Purity & Documentation

Purity: 98.59%

SDS (251 KB)

COA (246 KB) HNMR (121 KB) RP-HPLC (140 KB)

Handling Instructions (2659 KB)
References

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
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Rivoglitazone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rivoglitazone185428-18-6R-106056R106056R 106056PPARPeroxisome proliferator-activated receptorsUGT1A3hPPARαHT-1080 cellstype 2 diabetes mellitusCYP enzymesUGT2B7hPPARγhPPARδmale ZDF ratsmale db/db miceInhibitorinhibitorinhibit

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