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2-PMAP

Cat. No. M8471
2-PMAP Structure
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Biological Activity

2-PMAP is a brain penetrant inhibitor of amyloid precursor protein (APP) production. 2-PMAP lowers levels of the amyloid precursor protein (APP) in CHO APP751SW cells. Also it reduces brain level of APP in mice model. 2-PMAP exhibits no cellular toxicity up to 100 μM.

Chemical Information
Molecular Weight 200.24
Formula C12H12N2O
CAS Number 102212-26-0
Solubility (25°C) DMSO: 20 mg/mL
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] Chieh-Hsin Wu, et al. 2-PMAP Ameliorates Cerebral Vasospasm and Brain Injury after Subarachnoid Hemorrhage by Regulating Neuro-Inflammation in Rats

[2] Melanie D Balhuizen, et al. Outer Membrane Vesicles Protect Gram-Negative Bacteria against Host Defense Peptides

[3] Ayodeji A Asuni, et al. Modulation of amyloid precursor protein expression reduces β-amyloid deposition in a mouse model

[4] Andy Noble, et al. Doubly pyrazolate-bridged dinuclear complexes of a highly constrained bis-terdentate ligand: observation of a [high spin-low spin] state for [Fe(II)2(PMAP)2][SbF6]2.2.25(C3H8O) (PMAP = 3,5-bis{[N-(2-pyridylmethyl)amino]-methyl}-1H-pyrazolate)

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Keywords: 2-PMAP supplier, inhibitors, activators

 
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