SB408124 288150-92-5

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Molecular Weight: 356.37 SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a
functional antagonist of the OX1 receptor with a affinity of
approximately 50-fold selectivity over the OX2 receptor. A
recent study indicates that pretreatment of primary cultures of rat
astrocytes with SB-401824 before Orexin A administration significantly
reduced the stimulatory action of Orexin A on both basal and
forskolin-acivated cAMP production.

SB-408124 (30 μg/10 μL, administered intracerebroventricularly)
decreases Orexin-A induced water intake in Wistar rats.
Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the
vasopressin (VP) level increase induced by either histamine or 2.5%
NaCl administration, and this blocking effect is moderated by
pretreatment with SB-408124. Intracerebroventricular
pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline
(BIC)-induced increases in endogenous glucose production (EGP).
Protocol(Only for Reference)


Kinase Assay:


[1]

Whole cell binding assays

After overnight culture in 96-well Packard Cultur plates, the medium is discarded and cells are incubated in buffer containing 150 mM NaCl, 20 mM HEPES and 0.5% bovine serum albumin (pH 7.4) for 60 minutes at 25 °C. Saturation studies are carried out by incubating cells with a range of concentrations of [3H]SB-408124 (0.2–24 nM); the total assay volume is 250 μL. Protein content is assayed by lysing cells with 0.1M NaOH and using the Bradford method with bovine serum albumin (BSA) as a standard. Association kinetic studies are performed by measuring the specific binding of [3H]SB-408124 (3 nM) at 1–60 minutes after addition of [3H]SB-408124. All assays are terminated by washing the cells three times with 250μL ice-cold phosphate-buffered saline. A volume of 100 μL of Microscint 40 is added to each well and the plate is left at room temperature for 2 hours. Cell-associated radioactivity is then measured using a Packard Topcount, with a count time of 2 minute/well.

Membrane-based SPA binding assays

CHO-K1_OX1 cell membranes (75 μg/mL) are precoupled by shaking with wheatgerm-agglutinin polyvinyltoluene (WGA-PVT) scintillation proximity assay (SPA) beads (5 mg/mL) in buffer containing 25 mM HEPES, 2.5 mM MgCl2, 0.5 mM EDTA and 0.025% bacit

Animal Study:


[3]

Animal Models	Male Wistar rats
Formulation	SB-408124 is dissolved in saline.
Dosages	30 μg/10 μL
Administration	Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat.
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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)	356.37
Formula	C19H18F2N4O
CAS No.	288150-92-5

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

Solubility (25°C) *	In vitro	DMSO	36 mg/mL (101.01 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	30 mg/mL

Chemical Name	1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea

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Product Categories : Neuronal Signaling > OX Receptor Inhibitor