1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  2. Reactive Oxygen Species Mitochondrial Metabolism
  3. OPC-163493

OPC-163493 is an orally active and liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces the production of mitochondrial Δψ and ROS. OPC-163493 has anti-diabetic and lipid-lowering effects. In addition, OPC-163493 has a protective effect on cardiovascular disease.

For research use only. We do not sell to patients.

OPC-163493 Chemical Structure

OPC-163493 Chemical Structure

CAS No. : 1644467-84-4

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5 mg USD 296 In-stock
10 mg USD 475 In-stock
25 mg USD 960 In-stock
50 mg USD 1540 In-stock
100 mg USD 2465 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

OPC-163493 is an orally active and liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces the production of mitochondrial Δψ and ROS. OPC-163493 has anti-diabetic and lipid-lowering effects. In addition, OPC-163493 has a protective effect on cardiovascular disease[1][2].

In Vitro

OPC-163493 (0.5-10 μM; 15 min) inhibits the production of Δψ and ROS in isolated rat liver mitochondria[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

OPC-163493 (1 mg/kg; Oral administration; Single dose) is quickly absorbed and the peak plasma concentration reaches 0.393 μg/mL (1.17 μM), 3.5 h after administration, with a half-life of 3.74 h and bioavailability of 53.5% in rats[1].
OPC-163493 (1-10 mg/kg; Oral administration; 6 weeks) has an improved effect in diabetic rat model[1].
OPC-163493 (2-4 mg/kg; Oral administration; 2 weeks) has a lipid-lowering effect in rat models with high fat diet[1].
OPC-163493 (0.06% mixed chow; 51 days) has a protective effect in spontaneously hypertensive rat models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zucker diabetic fatty rats aged 11 weeks old[1]
Dosage: 1, 2, 4 and 10 mg/kg
Administration: Oral administration (p.o.); 6 weeks
Result: Suppressed HbA1c elevation in a dose-dependent manner.
Significantly lowered fasting blood glucose levels at doses of 4 and 10 mg/kg.
Had no significant effect on plasma insulin levels.
Animal Model: HFD SD rats aged 12 weeks old[1]
Dosage: 2 and 4 mg/kg
Administration: Oral administration (p.o.); 2 weeks
Result: Did not affect body weight and food intake during the treatment period.
Slightly but significantly reduced fasting blood glucose after 2-week treatment.
Significantly reduced hepatic total TG, total diacylglycerol (DAG), and total cholesterol ester (CE) by 57%, 25%, and 26%, respectively even in the low-dose group.
Significantly reduced long-chain acylcarnitines (AC, C16 and C18).
Animal Model: Salt-loaded stroke-prone spontaneously hypertensive rats (SHRSPs) aged 6 weeks old[1]
Dosage: 0.06% mixed chow
Administration: Oral administration (p.o.); 51 days
Result: Delayed stroke symptoms and death, lowered blood pressure.
Improved kidney function and urinary albumin-to-creatinine ratio, lowered uinary albumin excretion by 68%.
Molecular Weight

335.31

Formula

C14H8F3N5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C2=C(C)SC(C3=CC=C(C(F)(F)F)C=C3)=N2)N=NN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (372.79 mM; Need ultrasonic; 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 2.9823 mL 14.9116 mL 29.8231 mL
5 mM 0.5965 mL 2.9823 mL 5.9646 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
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 2.9823 mL 14.9116 mL 29.8231 mL 74.5579 mL
5 mM 0.5965 mL 2.9823 mL 5.9646 mL 14.9116 mL
10 mM 0.2982 mL 1.4912 mL 2.9823 mL 7.4558 mL
15 mM 0.1988 mL 0.9941 mL 1.9882 mL 4.9705 mL
20 mM 0.1491 mL 0.7456 mL 1.4912 mL 3.7279 mL
25 mM 0.1193 mL 0.5965 mL 1.1929 mL 2.9823 mL
30 mM 0.0994 mL 0.4971 mL 0.9941 mL 2.4853 mL
40 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8639 mL
50 mM 0.0596 mL 0.2982 mL 0.5965 mL 1.4912 mL
60 mM 0.0497 mL 0.2485 mL 0.4971 mL 1.2426 mL
80 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9320 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7456 mL
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  • 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.

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Product Name:
OPC-163493
Cat. No.:
HY-134769
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