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SB408124

Cat. No. M3324
SB408124 Structure
Size Price Availability
10mg USD 124  USD124 Out of stock
100mg USD 800  USD800 Out of stock
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Quality Control & Documentation
Biological Activity

SB-408124 is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70-fold selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334,867. It is used in scientific research into the function of orexinergic neurons in the body.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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.
Chemical Information
Molecular Weight 356.37
Formula C19H18F2N4O
CAS Number 288150-92-5
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] I Tissen, et al. OX1R ANTAGONIST SB408124 ACTION AND EXTRAHYPOTHALAMIC CRF IN RATS AFTER PSYCHOTRAUMATIC EXPOSURE

[2] Ying-Ying Tan, et al. Orexin Receptor-1 in the Rostral Ventrolateral Medulla Mediates the Antihypertensive Effects of Electroacupuncture

[3] Kouichi Yamamoto, et al. Activation of orexinergic and histaminergic pathway involved in therapeutic effect of histamine H 4 receptor antagonist against cisplatin-induced anorexia in mice

[4] Y Fan, et al. Orexin A increases sympathetic nerve activity through promoting expression of proinflammatory cytokines in Sprague Dawley rats

[5] Bao-Qiang Guo, et al. Cardiovascular effect of intracerebroventricular injection of orexin-1 receptor antagonist in rats

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  Catalog
Abmole Inhibitor Catalog




Keywords: SB408124 supplier, OX Receptor, inhibitors, activators


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