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ELN318463 racemate is a selective γ-secretase inhibitor, demonstrating differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase. It shows significant selectivity for PS1 with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. This compound acts as a classic γ-secretase inhibitor, inhibiting Aβ production with 75- to 120-fold selectivity over Notch signaling in cells.
Amyloid precursor protein (APP) selective γ-secretase inhibitor
Differentially inhibits presenilin (PS1) and PS2-comprised γ-secretase
51-fold more selective for PS1
Demonstrates 75- to 120-fold selectivity for inhibiting Aβ production
Displaces an active site-directed inhibitor in the presence of a substrate
Achieves brain levels up to 2.7 μM at 100 mg/kg dose
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Fluorofenidone (AKF-PD) is an orally active small-molecule research compound with reported anti-fibrotic, antioxidant, and anti-inflammatory effects. Supplied as a purified analytical standard suitable for in vitro and in vivo studies and commonly provided as a 50 mg pack.
Orally active small molecule with anti-fibrotic and anti-inflammatory activity.
Demonstrated cellular effects (e.g., NIH/3T3 IC50 ~2.75 mM) and in vitro activity in lung and cancer cell lines.
Shows protective effects in rodent models of lung injury, cholestasis, and fibrosis.
High purity suitable for analytical and preclinical research applications.
Molecular formula C12H10FNO; molecular weight 203.21 g/mol.
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Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor provided as a solid research compound for in vitro and in vivo studies. It is used to study COMT-mediated metabolism of L-DOPA and related pharmacology, and is supplied with characterization data and storage recommendations for experimental stability.
Reversible COMT inhibitor for research use.
Reported purity 99.9%.
Molecular weight 273.24 g/mol.
Physical form solid powder.
High solubility in DMSO (≥100 mg/mL) and formulated in vivo solubility ≥2.5 mg/mL in 10% DMSO/40% PEG300/5% Tween-80/45% saline.
Recommended storage 4°C protected from light; in solution store at -80°C up to 6 months or -20°C up to 1 month.
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C-021 is a small-molecule antagonist of CC chemokine receptor 4 (CCR4) developed for research applications; it blocks CCR4-mediated signaling and functional chemotaxis, with low-nanomolar activity in binding and cell-based assays.
Potent CCR4 antagonist with low-nanomolar binding activity.
Prevents CCL22-derived [35S]GTPγS binding to CCR4 (IC50 18 nM) and inhibits functional chemotaxis (human 140 nM, mouse 39 nM).
Molecular formula C27H41N5O2; molecular weight 467.65 g/mol.
High purity (~99.95%).
Solid form with recommended storage: powder -20°C (long term) or 4°C (short term); in solvent store at -80°C.
Intended for research use only; not for human use.
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PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. It may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects, and for targeted bone regeneration.
Potent and selective PYK2 inhibitor with an IC50 of 637 nM.
Promotes osteogenesis of hMSC cultures, increasing alkaline phosphatase (ALP) activity and mineralization.
Enhances osteoblast proliferation.
Enhances calcium deposition.
Increases cell proliferation activity in murine bone marrow-derived mesenchymal stem cells (BMSC).
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