Free shipping on all orders over $ 500

Leriglitazone

Cat. No. M21176
Leriglitazone Structure
Synonym:

Hydroxypioglitazone

Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) is a PPARγ agonist that provides high transcriptional potency by stabilizing the PPARγ (AF-2) coactivator binding surface and enhancing coactivator binding capacity. Leriglitazone (Hydroxypioglitazone) binds to PPARγC (LBD) with a Ki value of 1.2 μM and induces PPARγ (LBD) transcriptional efficiency with an EC50 of 680 nM.

Chemical Information
Molecular Weight 372.44
Formula C19H20N2O4S
CAS Number 146062-44-4
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ludger Schls. Lancet Neurol. Leriglitazone: frustration and hope in adrenoleukodystrophy

[2] Paolo Santambrogio, et al. Pharmaceutics. PPAR Gamma Agonist Leriglitazone Recovers Alterations Due to Pank2-Deficiency in hiPS-Derived Astrocytes

[3] Massimo Pandolfo, et al. Neurol Genet. Efficacy and Safety of Leriglitazone in Patients With Friedreich Ataxia: A Phase 2 Double-Blind, Randomized Controlled Trial (FRAMES)

[4] Laura Rodrguez-Pascau, et al. Sci Transl Med. The brain penetrant PPARγ agonist leriglitazone restores multiple altered pathways in models of X-linked adrenoleukodystrophy

[5] Laura Rodrguez-Pascau, et al. Neurobiol Dis. PPAR gamma agonist leriglitazone improves frataxin-loss impairments in cellular and animal models of Friedreich Ataxia

Related PPAR Products
AZD-9574

AZD-9574 is a potent blood-brain barrier permeability inhibitor of PARP1, showing > 8,000 times selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 selectively inhibits PARP1 at the SSB site. AZD-9574 is an anticancer compound that can be used in HRD+ breast cancer and advanced solid malignancies.

Balofloxacin Dihydrate

an agonist of the peroxisome proliferator-activated receptor delta (PPARd) signaling pathway

Choline Fenofibrate

Choline fenofibrate is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.

Saroglitazar Magnesium

Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

GW1929

GW1929 is a potent PPAR-γ agonist, with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: Leriglitazone, Hydroxypioglitazone supplier, PPAR, inhibitors, activators

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.