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A 438079

Cat. No. M11483
A 438079  Structure
Size Price Availability Quantity
10mg USD 122  USD122 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

A 438079 is A potent, selective P2X7 receptor antagonist with A pIC50 of 6.9.

Chemical Information
Molecular Weight 306.15
Formula C13H9Cl2N5
CAS Number 899507-36-9
Solubility (25°C) DMSO ≥ 60 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] Iven-Alex von Muecke-Heim, et al. Eur Arch Psychiatry Clin Neurosci. P2X7R antagonists in chronic stress-based depression models: a review

[2] Juliang Qin, et al. Cancer Immunol Res. Blocking P2X7-Mediated Macrophage Polarization Overcomes Treatment Resistance in Lung Cancer

[3] Nishkantha Arulkumaran, et al. Physiol Rep. P2X 7 receptor antagonism ameliorates renal dysfunction in a rat model of sepsis

[4] Wu Jiang, et al. J Neuroinflammation. Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice

[5] 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

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