| Bioactivity | TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo[1]. |
| Target | EC50: 9 nM (mGlu4 receptor)EC50: >10 μM (mGlu 1, 2, 3, 5, and 7 receptors) |
| Invitro | TC-N 22A is selected for mGlu4 and has an EC50 of 9 nM in human mGlu4-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC50>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC50 >10 μM) and shows low potential for hERG channel inhibition[1]. |
| In Vivo | TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats[1]. |
| Name | TC-N 22A |
| CAS | 1314140-00-5 |
| Formula | C14H13N5S |
| Molar Mass | 283.35 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sang-Phyo Hong, et al. Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. J Med Chem. 2011 Jul 28;54(14):5070-81. |