mk-1064

Product Name: mk-1064
CAS No.: 1207253-08-4
Chemical Name: mk-1064
Synonyms: CS-2221;mk-1064;MK1064;MK 1064;MK-1064, CID 44633765;MK-1064, 10 mM in DMSO;MK-1064(Urokinase inhibitor 1);5''-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide;5''-Chloro-N-((5,6-dimethoxypyridin-2-yl)methyl)-[2,2':5',3''-terpyridine]-3'-carboxamide;[2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-;5-(5-CHLOROPYRIDIN-3-YL)-N-[(5,6-DIMETHOXYPYRIDIN-2-YL)METHYL]-2-PYRIDIN-2-YLPYRIDINE-3-CARBOXAMIDE
CBNumber: CB43122022
Molecular Formula: C24H20ClN5O3
Formula Weight: 461.9
MOL File: 1207253-08-4.mol

More

Less

mk-1064 Property

Boiling point:: 662.4±55.0 °C(Predicted)
Density: 1.305±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:60.0(Max Conc. mg/mL);129.9(Max Conc. mM)
form: A crystalline solid
pka: 11.98±0.46(Predicted)
color: White to off-white

More

Less

Safety

HS Code: 2933399990

More

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More

Less

N-Bromosuccinimide Price

Cayman Chemical

Product number: 20993
Product name: MK-1064
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 20993
Product name: MK-1064
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 20993
Product name: MK-1064
Purity: ≥98%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 20993
Product name: MK-1064
Purity: ≥98%
Packaging: 25mg
Price: $618
Updated: 2024/03/01

ChemScene

Product number: CS-5968
Product name: MK-1064
Purity: 99.97%
Packaging: 1mg
Price: $108
Updated: 2021/12/16

More

Less

mk-1064 Chemical Properties,Usage,Production

Uses

MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia[1][3].

in vivo

MK-1064 (30?mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice^[2].
MK-1064 (30?mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats^[3].
MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey^[1].

Animal Model:	Wild-type and OX₂R knockout mice^[2]
Dosage:	30 mg/kg
Administration:	Oral administration
Result:	Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5?hours following treatment.

Animal Model:

Rat, dog, and rhesus monkey (Pharmacokinetics assay)^[1]

Dosage:

1, 2, 3, 5 mg/kg

Administration:

Oral administration (P.O.), intravenous injection (I.V.)

Result:

Pharmacokinetics profile of MK-1064.

Species	Dose (mg/kg)	CL (mL/min/kg)	t_1/2 (h)	Dose (mg/kg)	C_max (μM)	F (%)
Rat	2 (I.V.)	39	0.3	5 (P.O.)	1.5	54
Dog	1 (I.V.)	16	1.0	3 (P.O.)	1.0	48
Rhesus	2 (I.V.)	12	0.8	5 (P.O.)	0.9	16

IC 50

OX₂ Receptor: 18 nM (IC₅₀); OX₁ Receptor: 1789 nM (IC₅₀); OX₂ Receptor: 0.5 nM (Ki); OX₁ Receptor: 1584 nM (Ki)

References

[1] Roecker AJ 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. ChemMedChem. 2014 Feb;9(2):311-22. DOI:10.1002/cmdc.201300447
[2] Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. DOI:10.1038/srep27147
[3] Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323. DOI:10.1016/j.neuroscience.2017.02.038

mk-1064 Preparation Products And Raw materials

Raw materials

Preparation Products

More

Less

mk-1064 Suppliers

China 74 India 1 United States 8 Global 83

WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.

Tel: 17702719238 18971495150;
Email: sales@sun-shinechem.com
Country: China
ProdList: 1077
Advantage: 64

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4757
Advantage: 55

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9803
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9126
Advantage: 58

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973130 18101056239
Email: 3193328036@qq.com
Country: China
ProdList: 29760
Advantage: 68

Shanghai Resuperpharmtech Co., Ltd.

Tel: 02150565560; 17321237488
Email: kevin@resuperpharmtech.com
Country: China
ProdList: 356
Advantage: 58

Medi-tech Bioscientific Co., Ltd.

Tel: 0519-83246372 13585352506
Fax: 0519-83246372
Country: China
ProdList: 1844
Advantage: 58

1207253-08-4, mk-1064Related Search:

MK-2206 2HCl MK-5172 Mk-2461 . (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT Omarigliptin (MK-3102) MK-8998 MK-4101 MK8745 MK 0557 MK-0812 (Succinate) MKC9989 (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide MK-1775 SCH900776 MK-0752 MKC3946 MK-3903

mk-1064

5''-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide

MK-1064(Urokinase inhibitor 1)

5-(5-CHLOROPYRIDIN-3-YL)-N-[(5,6-DIMETHOXYPYRIDIN-2-YL)METHYL]-2-PYRIDIN-2-YLPYRIDINE-3-CARBOXAMIDE

MK-1064, CID 44633765

CS-2221

MK1064;MK 1064

[2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-

stress,MK1064,Orexin Receptor (OX Receptor),OX2R knockout,insomnia,Inhibitor,MK-1064,HCRT Receptor,Hypocretin Receptor,inhibit,Sleep

5''-Chloro-N-((5,6-dimethoxypyridin-2-yl)methyl)-[2,2':5',3''-terpyridine]-3'-carboxamide

MK-1064, 10 mM in DMSO

1207253-08-4