An orexin 2 receptor antagonist
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MK-1064

Item No. 20993

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-[2,2':5',3''-terpyridine]-3'-carboxamide
CAS Number
1207253-08-4
Molecular Formula
C24H20ClN5O3
Formula Weight
461.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 2.5 mg/ml
λmax
290 nm
SMILES
ClC1=CN=CC(C2=CN=C(C3=CC=CC=N3)C(C(NCC4=CC=C(OC)C(OC)=N4)=O)=C2)=C1
InChi Code
InChI=1S/C24H20ClN5O3/c1-32-21-7-6-18(30-24(21)33-2)14-29-23(31)19-10-16(15-9-17(25)13-26-11-15)12-28-22(19)20-5-3-4-8-27-20/h3-13H,14H2,1-2H3,(H,29,31)
InChi Key
CKTWQGHVNRYNCM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).1 It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roecker, A.J., Mercer, S.P., Schreier, J.D., et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. Chem. Med. Chem. 9(2), 311-322 (2014).

    2. Grafe, L.A., Eacret, D., Luz, S., et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience 348, 313-323 (2017).