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Arhalofenate

SKU: orb1308055

Description

Arhalofenate (JNJ 39659100) is a selective partial PPARγ agonist developed for type 2 diabetes research. It has been investigated in both in vitro assays and in vivo models for its potential to improve glycemic control and insulin sensitization.

Research Area

Metabolism Research, Molecular Biology

Images & Validation

Key Properties

CAS Number24136-23-0
MW415.79
Purity99.62%
FormulaC19H17ClF3NO4
SMILES[C@H](OC1=CC(C(F)(F)F)=CC=C1)(C(OCCNC(C)=O)=O)C2=CC=C(Cl)C=C2
TargetPPAR
SolubilityDMSO:132.5 mg/mL (318.67 mM)

Bioactivity

In Vivo
MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (60 mg/kg) causes a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels. Arhalofenate (100 mg/kg, p.o.) obviously increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (100 mg/kg, p.o.) significantly reduces triglyceride, free fatty acid, and cholesterol levels in ZDF rats. Arhalofenate (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats.
In Vitro
Arhalofenate displays a dose-dependent activation of mouse GAL4-PPAR-γ (EC50s: appr 12 μM). Arhalofenate is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. .

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Arhalofenate, inhibit, JNJ39659100, JNJ-39659100, JNJ 39659100, Inhibitor, MBX 102, MBX102, MBX-102, PPAR-γ, PPARγ, PPAR, Peroxisome proliferator-activated receptors

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Key Properties

No computed properties available.

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Arhalofenate (orb1308055)

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% DMSO +
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% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,300.00
5 mg
¥ 3,380.00
1 ml x 10 mM (in DMSO)
¥ 4,290.00
10 mg
¥ 5,460.00
25 mg
¥ 8,580.00
50 mg
¥ 11,830.00
100 mg
¥ 15,730.00
200 mg
¥ 21,060.00
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