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BioChemicals
AZD 9272
tcsc0033119
AZD 9272
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AVAILABLE SIZES
5mg
10mg
25mg
$
114.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
AZD 9272 is a brain penetrant
mGluR5
antagonist.
IC50 & Target: mGluR5
[1]
In Vitro:
AZD 9272 causes a concentration dependent decrease in the magnitude of the intracellular Ca
2+
response to 1.5 μM of the mGluR group I selective agonist DHPG in both the human and the rat mGluR5 expressing cell lines. The maximal inhibition is 100%. The mean IC
50
(±SD) value at the human mGluR5 is 7.6±1.1 nM (n=13) for AZD9272. The mean IC
50
value at the rat mGluR5 is 2.6±0.3 nM (n=3) for AZD9272. In contrast, 10 μM of AZD9272 does not diminish the response to 10 μM ATP in the background GHEK cells. Increasing concentrations of AZD9272 causes a decrease in the potency and the maximal response of DHPG. AZD9272 completely reverses the glutamate-stimulated (EC
80
, 80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with IC
50
of 26±3 nM (n=21)
[1]
.
In Vivo:
The clearance of AZD 9272 is low following a single intravenous dose at 3 μmol/kg and AZD 9272 is eliminated from plasma with terminal half-lives between 2 and 6 h. The terminal half-lives following oral dosing are similar to the half-lives following intravenous dosing. The volume of distribution at steady state is intermediate for AZD9272
[1]
. AZD9272 causes no cocaine-appropriate responding and causes a non-dose-dependent reduction in response rates at higher doses. AZD9272 at 2.84 mg/kg causes greater than 80% and typically more than 99% MTEP-appropriate responding up to 20 hours after dose, with a decline to approximately 20% at 24 hours after dose, yielding a t
1/2
of 21.93 hours, and causes no systematic effects on response rates. The first time point at which AZD9272 causes >90% MTEP-appropriate responding is at 30 minutes after dose
[2]
.
Information
CAS No
327056-26-8
Formula
C
14
H
6
F
2
N
4
O
Clinical Information
clinicalinformation
Pathway
GPCR/G Protein
Target
mGluR
Specifications
Purity / Grade
>98%
Solubility
10 mM in DMSO
Smiles
smiles
Misc Information
Observed Molecular Weight
284.22
related data
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