XAP044
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
XAP044 is a mGluR7 antagonist.
The function of metabotropic glutamate receptor subtype 7 (mGlu7), an critical presynaptic regulator of neurotransmission in the mammalian CNS, has been linked to drug abuse, anxiety, autism, as well as depression. However, it is difficult to develop specific blockers of native mGlu7 signaling in relevant brain areas such as limbic cortex and amygdala.
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].
Clinical trial: Up to now, XAP044 is still in the preclinical development stage.
Reference:
[1] C. E. Gee, D. Peterlik, C. Neuh user, et al. Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. The Journal of Biological Chemisty 289(16), 10975-10987 (2014).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 380.1 |
Cas No. | 196928-50-4 |
Formula | C15H9IO4 |
Solubility | ≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | 7-hydroxy-3-(4-iodophenoxy)-4H-1-benzopyran-4-one |
SDF | Download SDF |
Canonical SMILES | O=C1C2=CC=C(O)C=C2OC=C1OC3=CC=C(I)C=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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