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A 438079 hydrochloride

Cat. No. M11482
A 438079 hydrochloride  Structure
Synonym:

A-438079 HCl

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

Chemical Information
Molecular Weight 342.611
Formula C13H10Cl3N5
CAS Number 899431-18-6
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage 4°C , dry , sealed
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] Juliang Qin, et al. Cancer Immunol Res. Blocking P2X7-Mediated Macrophage Polarization Overcomes Treatment Resistance in Lung Cancer

[2] Jess Snchez-Nogueiro, et al. Eur J Pharmacol. Subcellular distribution and early signalling events of P2X7 receptors from mouse cerebellar granule neurons

[3] Kimiko Kobayashi, et al. Neurosci Lett. Induction of the P2X7 receptor in spinal microglia in a neuropathic pain model

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