MNI 137Selective negative allosteric modulator of group II mGlu receptors CAS# 946619-21-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 946619-21-2 | SDF | Download SDF |
| PubChem ID | 25210562 | Appearance | Powder |
| Formula | C15H9BrN4O | M.Wt | 341.16 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | 4-(8-bromo-2-oxo-1,3-dihydro-1,5-benzodiazepin-4-yl)pyridine-2-carbonitrile | ||
| SMILES | C1C(=NC2=C(C=C(C=C2)Br)NC1=O)C3=CC(=NC=C3)C#N | ||
| Standard InChIKey | KMKZCMKOSAKVGY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H9BrN4O/c16-10-1-2-12-14(6-10)20-15(21)7-13(19-12)9-3-4-18-11(5-9)8-17/h1-6H,7H2,(H,20,21) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective negative allosteric modulator of group II mGlu receptors (IC50 values are 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization). Displays no activity at mGlu1, mGlu4, mGlu5 or mGlu8 receptors in a calcium mobilization assay. |
MNI 137 Dilution Calculator
MNI 137 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9312 mL | 14.6559 mL | 29.3118 mL | 58.6235 mL | 73.2794 mL |
| 5 mM | 0.5862 mL | 2.9312 mL | 5.8624 mL | 11.7247 mL | 14.6559 mL |
| 10 mM | 0.2931 mL | 1.4656 mL | 2.9312 mL | 5.8624 mL | 7.3279 mL |
| 50 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.1725 mL | 1.4656 mL |
| 100 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.5862 mL | 0.7328 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors.[Pubmed:17416742]
J Pharmacol Exp Ther. 2007 Jul;322(1):254-64.
Group II metabotropic glutamate receptors (mGluRs), mGluR2 and mGluR3, play a number of important roles in mammalian brain and represent exciting new targets for certain central nervous system disorders. We now report synthesis and characterization of a novel family of derivatives of dihydrobenzo[1,4]diazepin-2-one that are selective negative allosteric modulators for group II mGluRs. These compounds inhibit both mGluR2 and mGluR3 but have no activity at group I and III mGluRs. The novel mGluR2/3 antagonists also potently block mGluR2/3-mediated inhibition of the field excitatory postsynaptic potentials at the perforant path synapse in hippocampal slices. These compounds induce a rightward shift and decrease the maximal response in the glutamate concentration-response relationship, consistent with a noncompetitive antagonist mechanism of action. Furthermore, radioligand binding studies revealed no effect on binding of the orthosteric antagonist [(3)H]LY341495 [2S-2-amino-2-(1S,2S-2-carboxycyclopropan-1-yl)-3-(xanth-9-yl)propionic acid]. Site-directed mutagenesis revealed that a single point mutation in transmembrane V (N735D), previously shown to be an important residue for potentiation activity of the mGluR2 allosteric potentiator LY487379 [N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethyla mine], is not critical for the inhibitory activity of negative allosteric modulators of group II mGluRs. However, this single mutation in human GluR2 almost completely blocked the enhancing activity of biphenyl-indanone A, a novel allosteric potentiator of mGluR2. Our data suggest that these two positive allosteric modulators of mGluR2 may share a common binding site and that this site may be distinct from the binding site for the new negative allosteric modulators of group II mGluRs.
