| Company Name: |
Musechem |
| Tel: |
+1-800-259-7612 |
| Email: |
info@musechem.com |
|
| | MRK-016 Basic information |
| Product Name: | MRK-016 | | Synonyms: | 7-(5-Methyl-1,2-oxazol-3-yl)-3-(2-methyl-2-propanyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazine;MRK016;MRK 016;3-[3-tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazole;Pyrazolo[1,5-d][1,2,4]triazine, 3-(1,1-dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-;3-(9-(tert-Butyl)-8-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazin-2-yl)-5-methylisoxazole | | CAS: | 342652-67-9 | | MF: | C17H20N8O2 | | MW: | 368.39 | | EINECS: | | | Product Categories: | | | Mol File: | 342652-67-9.mol |  |
| | MRK-016 Chemical Properties |
| Melting point | 175-176 °C(Solv: ethyl ether (60-29-7); methanol (67-56-1)) | | density | 1.43±0.1 g/cm3(Predicted) | | storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | DMF: 2 mg/ml; DMSO: Slightly soluble; Ethanol: Slightly soluble; PBS (pH 7.2): 0.2 mg/ml | | form | A solid | | pka | 2.28±0.10(Predicted) | | color | White to off-white | | InChI | 1S/C17H20N8O2/c1-10-6-11(23-27-10)15-21-19-7-12-14(17(2,3)4)16(22-25(12)15)26-8-13-18-9-20-24(13)5/h6-7,9H,8H2,1-5H3 | | InChIKey | QYSYOGCIDRANAR-UHFFFAOYSA-N | | SMILES | CC(C)(C1=C2C=NN=C(N2N=C1OCC3=NC=NN3C)C4=NOC(C)=C4)C |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | MRK-016 Usage And Synthesis |
| Uses | MRK 016 is an inverse benzodiazepine antagonist which may assist in mitigating inflammation-induced decrements in cognitive function. | | Biological Activity | MRK-016 is an orally active, benzodiazepine site-targeting, alpha5-selective GABAA inverse agonist (Emax = -55%/α5, -16%/α1, -9%/α3, +6%/α2 of a EC20 GABA response using respective recombinant human αβ3γ2) with in vivo cognition-enhancing properties (0.3-3 mg/kg p.o. in r at Morris water maze test). | | in vivo | MRK-016 does not enhance pentylenetetrazole-induced convulsions at 10 mg/kg via ip, or cause seizures at 30 mg/kg, via po for 20 days in mice. MRK-016 shows no obvious anxiogenic-like effects in rats at doses that occupy >95% of benzodiazepine (BZ) binding sites. MRK-016 (0.3, 1, and 3 mg/kg, p.o.) dose-dependently improves performance of rats hippocampal-dependent memory task[1]. MRK-016 (0.3-30 mg/kg, p.o.) causes good receptor occupancy in rats. MRK-016 (0.3, 1, or 3 mg/kg p.o.) shows cognition-enhancing activity in the delayed matching-to-position version of the Morris water maze. MRK-016 (1, 3, or 10 mg/kg i.p.) does not produce kindling in mice[2]. MRK-016 (3 mg/kg, i.p.) protects against LPS-induced learning/memory decrements in mice[3]. | | storage | Store at +4°C |
| | MRK-016 Preparation Products And Raw materials |
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