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GW 791343 hydrochloride

Cat. No. M1909
GW 791343 hydrochloride Structure
Size Price Availability Quantity
10mg USD 135 In stock
50mg USD 540 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GW 791343 hydrochloride is a P2X7 allosteric modulator (pIC50 = 6.9 - 7.2). Chimeric human-rat P2X(7) receptors were constructed with regions of the rat receptor being inserted into the human receptor. Antagonist effects at these receptors were measured in ethidium accumulation and radioligand binding studies. GW 791343 hydrochloride exhibits negative allosteric effects at the human P2X(7) receptor but is a positive allosteric modulator of rat P2X(7). GW791343 can significantly affect agonist potency at the P2X(7) receptor by its predominant effect. Further studies, in which single amino acids were exchanged, identified amino acid 95 as being primarily responsible for the differential allosteric effects of GW791343.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 483.81
Formula C20H24F2N4O.3HCl
CAS Number 1019779-04-4
Purity >99%
Solubility DMSO
Water
Storage at -20°C
References

Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.
Michel AD, et al. Br J Pharmacol. 2008 Nov;155(5):738-51. PMID: 18660826.

Negative and positive allosteric modulators of the P2X(7) receptor.
Michel AD, et al. Br J Pharmacol. 2008 Feb;153(4):737-50. PMID: 18071294.

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  Catalog
Abmole Inhibitor Catalog 2017




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