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BOC Sciences
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1-631-485-4226; 16314854226 |
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| Products Intro: |
Product Name:XAP 044
CAS:196928-50-4
Purity:98% by HPLC Remarks:XAP 044 is a potent, selective and brain penetrating mGlu7 antagonist (IC50 = 88 nM). It inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. XAP 044 exhibits an
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| Company Name: |
Block Chemical Technology (Shanghai) Co., LTD
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021-20432219 13918097649 |
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li_jinfei@acblock-lab.com |
| Products Intro: |
Product Name:7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one
CAS:196928-50-4
Purity:0.95 Package:5g,250g,1kg Remarks:4.936
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| Product Name: | XAP044 | | Synonyms: | XAP044;7-Hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one;4H-1-Benzopyran-4-one, 7-hydroxy-3-(4-iodophenoxy)-;7-Hydroxy-3-(4-iodophenoxy)-4H-1-benzopyran-4-one;XAP-044,mGlu7,XAP044,neurotransmission,brain exposure,CNS,inhibit,mGluR,antidepressant,Metabotropic glutamate receptors,wide spectrum,anti-stress,Inhibitor,anxiolytic-like,XAP 044 | | CAS: | 196928-50-4 | | MF: | C15H9IO4 | | MW: | 380.13 | | EINECS: | | | Product Categories: | | | Mol File: | 196928-50-4.mol |  |
| | XAP044 Chemical Properties |
| Boiling point | 485.7±45.0 °C(Predicted) | | density | 1.853±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | | form | crystalline solid | | pka | 6.70±0.20(Predicted) |
| | XAP044 Usage And Synthesis |
| Description | XAP044 is an antagonist of the metabotropic glutamate (mGlu) receptor 7 (mGluR7), inhibiting lateral amygdala long term potentiation in brain slices from wild-type mice with an IC50 value of 88 nM. This effect is absent in mGluR7-deficient mice. XAP044 demonstrates good brain penetrance, producing wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral tests. | | Uses | XAP 044 is a potent mGlu7 antagonist used in the treatment of anxiety and depression in mice (1,2). Applications towards stress, autism and drug abuse are also potential uses. | | 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]. | | storage | -20°C | | references | [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). |
| | XAP044 Preparation Products And Raw materials |
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