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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
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 306.15
Formula C13H9Cl2N5
CAS Number 899507-36-9
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
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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