Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 56.00 | |
2 mg | In stock | $ 79.00 | |
5 mg | In stock | $ 115.00 | |
10 mg | In stock | $ 218.00 | |
25 mg | In stock | $ 389.00 | |
50 mg | In stock | $ 587.00 | |
100 mg | In stock | $ 839.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 157.00 |
Description | XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1]. |
In vitro | Previous study showed that in contrast to all previous mGlu7-selective drugs, XAP044 did not act through the seven-transmembrane region but rather via a binding pocket localized in mGlu7's extracellular Venus flytrap domain, a region identified for orthosteric agonist binding, which was suggested by the chimeric receptor studies in recombinant cell line assays [1]. |
In vivo | In rodent behavioral paradigms, XAP044 demonstrated good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy. In addition, XAP044 could reduce freezing during acquisition of Pavlovian fear and innate anxiety, which was consistent with the phenotypes of mGlu7-deficient mice. Moreover, XAP044 was able to inhibit lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm. It was alos found that there was no effect of XAP044 on LTP of mGlu7-deficient mice, suggesting that such pharmacological effect was mGlu7-dependent [1]. |
Molecular Weight | 380.13 |
Formula | C15H9IO4 |
CAS No. | 196928-50-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (157.84 mM)
You can also refer to dose conversion for different animals. More
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XAP044 196928-50-4 Neuroscience GluR mGlu7 neurotransmission brain exposure CNS XAP-044 inhibit mGluR antidepressant Metabotropic glutamate receptors wide spectrum XAP 044 anti-stress Inhibitor anxiolytic-like inhibitor