MMPIP hydrochloridePotent, allosteric mGlu7-selective antagonist CAS# 479077-02-6 |
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Quality Control & MSDS
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| Cas No. | 479077-02-6 | SDF | Download SDF |
| PubChem ID | 9945530 | Appearance | Powder |
| Formula | C19H15N3O3 | M.Wt | 333.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO | ||
| Chemical Name | 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-yl-[1,2]oxazolo[4,5-c]pyridin-4-one | ||
| SMILES | CN1C(=CC2=C(C1=O)C(=NO2)C3=CC=NC=C3)C4=CC=C(C=C4)OC | ||
| Standard InChIKey | PDWYBOZNEVALOV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H15N3O3/c1-22-15(12-3-5-14(24-2)6-4-12)11-16-17(19(22)23)18(21-25-16)13-7-9-20-10-8-13/h3-11H,1-2H3 | ||
| 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 | Potent allosteric mGlu7-selective receptor antagonist. Inhibits agonist-induced intracellular calcium mobilization and cAMP accumulation (IC50 values are 26 and 610 nM). Displays intrinsic activity; increases forskolin-induced cAMP accumulation in the absence of an agonist (IC50 = 15 nM), indicating inverse agonist activity. |
MMPIP hydrochloride Dilution Calculator
MMPIP hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0003 mL | 15.0015 mL | 30.003 mL | 60.006 mL | 75.0075 mL |
| 5 mM | 0.6001 mL | 3.0003 mL | 6.0006 mL | 12.0012 mL | 15.0015 mL |
| 10 mM | 0.3 mL | 1.5002 mL | 3.0003 mL | 6.0006 mL | 7.5008 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6001 mL | 1.2001 mL | 1.5002 mL |
| 100 mM | 0.03 mL | 0.15 mL | 0.3 mL | 0.6001 mL | 0.7501 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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In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists.[Pubmed:17609420]
J Pharmacol Exp Ther. 2007 Oct;323(1):147-56.
Novel isoxazolopyridone derivatives that are metabotropic glutamate receptor (mGluR) 7 antagonists were discovered and pharmacologically characterized. 5-Methyl-3,6-diphenylisoxazolo[4,5-c]pyridin-4(5H)-one (MDIP) was identified by random screening, and 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-ylisoxazolo[4,5-c]pyridin-4(5H)-one (MMPIP) was produced by chemical modification of MDIP. MDIP and MMPIP inhibited L-(+)-2-amino-4-phosphonobutyric acid (L-AP4)-induced intracellular Ca2+ mobilization in Chinese hamster ovary (CHO) cells coexpressing rat mGluR7 with Galpha(15) (IC50 = 20 and 26 nM). The maximal response in agonist concentration-response curves was reduced in the presence of MMPIP, and its antagonism is reversible. MMPIP did not displace [3H](2S)-2-amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid (LY341495) bound to mGluR7. These results suggested that these isoxazolopyridone derivatives are allosteric antagonists. In CHO cells expressing rat mGluR7, MDIP and MMPIP inhibited l-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC50 = 99 and 220 nM). In CHO cells coexpressing human mGluR7 with Galpha(15), MDIP and MMPIP also inhibited the l-AP4-induced cAMP response. The maximal degree of inhibition by MMPIP was higher than that by MDIP in a cAMP assay. MMPIP was able to antagonize an allosteric agonist, the N,N'-dibenzhydryl-ethane-1,2-diamine dihydrochloride (AMN082)-induced inhibition of cAMP accumulation. In the absence of these agonists, MMPIP caused a further increase in forskolin-stimulated cAMP levels in CHO cells expressing mGluR7, whereas a competitive antagonist, LY341495, did not. This result indicates that MMPIP has an inverse agonistic activity. The intrinsic activity of MMPIP was pertussis toxin-sensitive and mGluR7-dependent. MMPIP at concentrations of at least 1 microM had no significant effect on mGluR1, mGluR2, mGluR3, mGluR4, mGluR5, and mGluR8. MMPIP is the first allosteric mGluR7-selective antagonist that could potentially be useful as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions.
