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.
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Chemical Information
| Name | MK-8189 |
|---|---|
| Iupac Chemical Name | 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 |
| Synonyms | MK-8189; MK8189; MK 8189 |
| Molecular Formula | C19H22N6OS |
| Molecular Weight | 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 Number | 1424371-93-6 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
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| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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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.
Chemical Structure
