- ADX88178
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- $53.00 / 5mg
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2024-11-19
- CAS:1235318-89-4
- Min. Order:
- Purity: 99.55%
- Supply Ability: 10g
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| | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- Basic information |
| Product Name: | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- | | Synonyms: | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-;5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine;4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-2-Pyrimidinamine;ADX88178;ADX-88178;5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine;ADX88178, >98%;ADX-88178;ADX 88178;ADX88178 | | CAS: | 1235318-89-4 | | MF: | C12H12N6S | | MW: | 272.33 | | EINECS: | | | Product Categories: | | | Mol File: | 1235318-89-4.mol | ![2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- Structure](CAS/GIF/1235318-89-4.gif) |
| | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:16.67(Max Conc. mg/mL);61.21(Max Conc. mM) | | form | Solid | | color | White to off-white |
| | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- Usage And Synthesis |
| Description | ADX-88178 is a novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4 receptor in rodent models of anxiety, obsessive compulsive disorder (OCD), fear, depression, and psychosis. ADX88178 dose-dependently reduced the number of buried marbles in the marble burying test and increased open-arm exploration in the elevated plus maze (EPM) test, indicative of anxiolytic-like efficacy. | | Uses | ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4. | | in vivo | In mice, ADX88178 (1-30 mg/kg p.o.) dose-dependently increases the number of open-arm entries. Specifically, at 3, 10, and 30 mg/kg ADX88178, there are 5-, 7-, and almost 13-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 3, 10, and 30 mg/kgADX88178, there are 8-, 12-, and 24-fold increases in the time spent in the open arms when compared with the vehicle-treated controls. In rats, ADX88178 (10-100 mg/kg p.o.) dose-dependently increases the number of open-arm entries in the rat EPM test. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 5-, 8-, and more than 10-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 7.5-, 11-, and 13-fold increases in time spent in the open arms when compared with the vehicle-treated controls[3]. | | target | ADX88178 is a metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4. | | IC 50 | mGluR4: 4 nM (EC50) | | References | [1] Fujinaga M, et al. Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). Bioorg Med Chem L DOI:10.1016/j.bmcl.2015.12.008
[2] Ponnazhagan R, et al. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol. 2016 Jun;11(2):231-7. DOI:10.1007/s11481-016-9655-z
[3] Kalinichev M, et al. Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders. J Pharmacol Exp Ther. 2014 Sep;350(3):495-505. DOI:10.1124/jpet.114.214437 |
| | 2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- Preparation Products And Raw materials |
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