Suvorexant (MK-4305) 1030377-33-3

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Molecular Weight: 450.92 Suvorexant (MK-4305) is a potent dual OX receptor antagonist with Ki of 0.55 nM and 0.35 nM for OX1 receptor and OX2 receptor, respectively. Phase 3.

Suvorexant has excellent passive permeability and oral bioavailability, and induces favorable sleep effects in rats. In addition, suvorexant significantly and dose-dependently reduces
locomotor activity and promotes sleep in rats (10, 30, and 100 mg/kg),
dogs (1 and 3 mg/kg), and rhesus monkeys (10 mg/kg).

Protocol(Only for Reference)

Kinase Assay: [1]

FLIPR Assay

For intracellular calcium measurements, Chinese hamster ovary (CHO) cells expressing the Ile408-Val variant of the orexin 1 receptor or the human orexin 2 receptor, are grown in Iscove`s modified DMEM containing 2 mM l-glutamine, 0.5 g/mL G418, 1% hypoxanthine-thymidine supplement, 100 U/mL penicillin, 100 ug/mL streptomycin, and 10% heat-inactivated fetal calf serum. The cells are seeded at 20000 cells/well into Becton-Dickinson black 384-well clear bottom sterile plates coated with poly-d-lysine. All reagents are from GIBCO-Invitrogen Corp. The seeded plates are incubated overnight at 37 °C and 6% CO2. Ala-6,12 human orexin-A as the agonist is prepared as a 0.5 mM stock solution in 1% bovine serum albumin (BSA) and diluted in assay buffer (HBSS containing 20 mM HEPES and 2.5 mM probenecid, pH 7.4) for use in the assay at a final concentration of 0.3−2 nM. Test compounds are prepared as 10 mM stock solution in DMSO, then diluted and pipetted in 384-well plates, first in DMSO, then assay buffer. On the day of the assay, cells are washed three times with 100 μL assay buffer and then incubated for 60 min (37 °C, 6% CO2) in 60 μL of assay buffer containing 1 μM Fluo-4AM ester, 0.02% pluronic acid, and 1% BSA. The dye loading solution is then aspirated and cells washed three times with 100 μL of assay buffer. Then 30 μL of that same buffer is left in each well. Within the fluorescent imaging plate reader, test compounds are added to the plate in a volume of 15 μL, incubated for 5 min, and finally 15 μL of agonist is added. Fluorescence is measured for each well at 1 s intervals for 1 min and at 6 s intervals for 4 min, and the height of each fluorescence peak is compared to the height of the fluorescence peak induced by 0.3−2 nM Ala-6,12 orexin-A with buffer in place of antagonist. For each antagonist, the IC50 value (the concentration of compound needed to inhibit 50% of the agonist response) is determined.

Animal Study: [1]

Animal Models	Adult male Sprague−Dawley rats
Formulation	20% aqueous solution of TPGS
Dosages	~10 mg/kg
Administration	Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	450.92
Formula	C23H23ClN6O2
CAS No.	1030377-33-3

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	10 mg/mL (22.17 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (

Chemical Name	5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole

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Product Categories : Neuronal Signaling > OX Receptor Inhibitor