| Bioactivity | MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability. |
| Target | IC50:9.6 nM(mGluR2) |
| Invitro | MK-8768 (40 n M, 5 min) 在过表达 mGluR2 的 CHOdhfr 细胞系中抑制 mGluR2 酶活，IC50值为0.9 nM[1]。 Cell Viability Assay Cell Line: |
| In Vivo | MK-8768 优先采用肌肉注射[1]。MK-8768 (3 mg/kg, i.m, 2 times weekly) 在恒河猴ORD模型中明显改善东莨菪碱损伤后的影响，维持良好的执行功能和注意力[1]。 Animal Model: |
| Name | MK-8768 |
| CAS | 1432729-22-0 |
| Formula | C21H22F3N5O2 |
| Molar Mass | 433.43 |
| 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]. Michael T. Rudd, et al. Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator. ACS Med. Chem. Lett.. 2023，14，8. [2]. Sean M Smith, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.Neuropharmacology, 2013 Jan;64:215-23. |
MK-8768
CAS: 1432729-22-0 F: C21H22F3N5O2 W: 433.43
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .
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