GSK 1997132B
GSK 1997132B is a benzimidazole-based PPARγ partial agonist that can cross the blood-brain barrier with a pEC50 value of 8.0. GSK 1997132B has no significant effect on PPARα/δ. GSK 1997132B improves the problem of high blood clearance rate of earlier compounds, avoiding side effects such as weight gain and edema. GSK 1997132B can be used for research on Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 1168138-37-1
- Formula: C24H22F2N4O
- Molecular Weight:420.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PPAR-γ 8 (pEC50) |
Chemical Information
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CAS No. 1168138-37-1
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Molecular Weight 420.45
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Formula C24H22F2N4O
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SMILES
O=C(N[C@H](CC)C1=CC=CC=C1)C2=CC=C3N(C(C)=NC3=C2)CC4=NC=C(C=C4F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
[1]. Sime M, et al. Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5568-72. doi: 10.1016/j.bmcl.2011.06.088. Epub 2011 Jun 29. Erratum in: Bioorg Med Chem Lett. 2013 Feb 15;23(4):1143. Wilson, Timothy M [corrected to Willson, Timothy M]. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)