MedKoo Cat#: 122513 | Name: MK-8189

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

MK-8189
MK-8189
CAS#1424371-93-6 (SS-isomer)

Theoretical Analysis

MedKoo Cat#: 122513

Name: MK-8189

CAS#: 1424371-93-6 (SS-isomer)

Chemical Formula: C19H22N6OS

Exact Mass: 382.1600

Molecular Weight: 382.49

Elemental Analysis: C, 59.66; H, 5.80; N, 21.97; O, 4.18; S, 8.38

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1424378-99-3 (RR-isomer) 1424371-93-6 (SS-isomer)
Synonym
MK-8189; MK8189; 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
InChi Key
WQKPZDLZRFTMTI-CABCVRRESA-N
InChi Code
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
SMILES Code
CC1=NN=C(CNC2=NC(C)=NC(OC[C@@H]3[C@@H](C4=NC=C(C)C=C4)C3)=C2)S1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 382.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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.