MK-8189
MK-8189 is a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia. MK-8189 exhibited moderate plasma clearance and relatively low volume of distribution in rats and rhesus monkeys, resulting in a half-life of 4.8 h in rats and 4.2 h in rhesus monkeys. Oral bioavailability ranged from 41% in rhesus monkeys to 46% in rats. MK-8189 has an excellent profile against ion channels (Iks, Cav1.2, and Nav1.5 > 30 μM, and functional hERG Ikr IC50 = 33 μM). MK-8189 was efficacious in a test of episodic memory, the novel objection recognition assay in rats.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | MK-8189 |
|---|---|
| Iupac 化学名称 | 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine |
| 同义词 | MK-8189; MK8189; MK 8189 |
| 英文同义词 | MK-8189; MK8189; MK 8189 |
| 分子式 | C19H22N6OS |
| 分子量 | 382.48 |
| Smile | CC1=NN=C(CNC2=NC(C)=NC(OC[C@@H]3[C@@H](C4=NC=C(C)C=C4)C3)=C2)S1 |
| InChiKey | WQKPZDLZRFTMTI-CABCVRRESA-N |
| InChi | InChI=1S/C19H22N6OS/c1-11-4-5-16(20-8-11)15-6-14(15)10-26-18-7-17(22-12(2)23-18)21-9-19-25-24-13(3)27-19/h4-5,7-8,14-15H,6,9-10H2,1-3H3,(H,21,22,23)/t14-,15+/m1/s1 |
| Cas号 | 1424371-93-6 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Krogmann A, Peters L, von Hardenberg L, Bödeker K, Nöhles VB, Correll CU. Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities. CNS Spectr. 2019 Aug;24(S1):38-69. doi: 10.1017/S109285291900124X. PMID: 31482779.
2: Lobo MC, Whitehurst TS, Kaar SJ, Howes OD. New and emerging treatments for schizophrenia: a narrative review of their pharmacology, efficacy and side effect profile relative to established antipsychotics. Neurosci Biobehav Rev. 2022 Jan;132:324-361. doi: 10.1016/j.neubiorev.2021.11.032. Epub 2021 Nov 24. PMID: 34838528.
3: Layton ME, Kern JC, Hartingh TJ, Shipe WD, Raheem I, Kandebo M, Hayes RP, Huszar S, Eddins D, Ma B, Fuerst J, Wollenberg GK, Li J, Fritzen J, McGaughey GB, Uslaner JM, Smith SM, Coleman PJ, Cox CD. Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia. J Med Chem. 2023 Jan 9. doi: 10.1021/acs.jmedchem.2c01521. Epub ahead of print. PMID: 36624931.
