A 438079 is A potent, selective P2X7 receptor antagonist with A pIC50 of 6.9.
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Iven-Alex von Muecke-Heim, et al. Eur Arch Psychiatry Clin Neurosci. P2X7R antagonists in chronic stress-based depression models: a review
 Juliang Qin, et al. Cancer Immunol Res. Blocking P2X7-Mediated Macrophage Polarization Overcomes Treatment Resistance in Lung Cancer
 Nishkantha Arulkumaran, et al. Physiol Rep. P2X 7 receptor antagonism ameliorates renal dysfunction in a rat model of sepsis
 Wu Jiang, et al. J Neuroinflammation. Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice
 Daniel Marcellino, et al. J Neural Transm (Vienna). On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079
AS1411 is a quadruplex-forming oligonucleotide aptamer that targets nucleolin. AS1411 has anti-tumor activity.
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB).
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP. MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.
|Methuosis inducer 1
Methuosis inducer 1 is a potent methuosis inducer. Methuosis inducer 1 has anticancer activity.
|Dextran (Mw 150000)
Dextran is a multipurpose branched glucan, which can improve plasma colloid osmotic pressure, increase blood volume, reduce platelet adhesion, inhibit red blood cell aggregation, reduce blood viscosity, reduce peripheral circulation resistance, and unclog microcirculation.
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