| Cas No.: | 1235318-89-4 |
| Chemical Name: | 4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-2-Pyrimidinamine |
| Synonyms: | 4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-2-Pyrimidinamine;ADX88178;5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4- yl)thiazol-2-amine;2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]- |
| SMILES: | CC1=C(C2=CNN=C2)N=C(NC3=NC=CC(C)=N3)S1 |
| Formula: | C12H12N6S |
| M.Wt: | 272.328879356384 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4. |
| In Vivo: | ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. ADX88178 is used as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). ADX88178 potentiates glutamate-mediated activation of human mGluR4 with EC50 values of 4 nM without significant effects on other mGluRs (EC50 > 30 μM)[1]. ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4. Microglia are pretreated with 1, 10 or 100 nM ADX88178 or 100 nM LAP4 for 30 min followed by LPS treatment for 24 h prior to collecting culture supernatant for ELISA measurement of TNFα levels. The pre-treatment with ADX88178 and LAP4 both significantly attenuate LPS-induced TNFα levels. As little as 1 nM of ADX88178 is sufficient to inhibit TNFα, and is as effective at concentrations of 10 and 100 nM[2]. |
| In Vitro: | ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. ADX88178 is used as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). ADX88178 potentiates glutamate-mediated activation of human mGluR4 with EC50 values of 4 nM without significant effects on other mGluRs (EC50 > 30 μM)[1]. ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4. Microglia are pretreated with 1, 10 or 100 nM ADX88178 or 100 nM LAP4 for 30 min followed by LPS treatment for 24 h prior to collecting culture supernatant for ELISA measurement of TNFα levels. The pre-treatment with ADX88178 and LAP4 both significantly attenuate LPS-induced TNFα levels. As little as 1 nM of ADX88178 is sufficient to inhibit TNFα, and is as effective at concentrations of 10 and 100 nM[2]. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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