product name VU 0357121
Description: VU0357121 is a novel and highly selective positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. Mutagenesis studies indicate that VU0357121 and related analogues bind to a yet uncharacterized allosteric site on mGlu(5), distinct from CPPHA, yet share a functional interaction with the MPEP site.
References: ACS Chem Neurosci. 2010 Oct 20;1(10):702-716; Mol Pharmacol. 2012 Nov;82(5):860-75.
305.32
Formula
C17H17F2NO2
CAS No.
433967-28-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 61 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 21 mg/mL (68.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423537
| In Vitro |
In vitro activity: VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Chem Neurosci. 2010 Oct 20;1(10):702-716; Mol Pharmacol. 2012 Nov;82(5):860-75. |
