XAP044 |
Catalog No.GC18120 |
XAP044 es un antagonista potente y selectivo de mGlu7.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 196928-50-4
Sample solution is provided at 25 µL, 10mM.
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).
Cas No. | 196928-50-4 | SDF | |
Chemical Name | 7-hydroxy-3-(4-iodophenoxy)-4H-1-benzopyran-4-one | ||
Canonical SMILES | O=C1C2=CC=C(O)C=C2OC=C1OC3=CC=C(I)C=C3 | ||
Formula | C15H9IO4 | M.Wt | 380.1 |
Solubility | ≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.6309 mL | 13.1544 mL | 26.3089 mL |
5 mM | 0.5262 mL | 2.6309 mL | 5.2618 mL |
10 mM | 0.2631 mL | 1.3154 mL | 2.6309 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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