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SB-334867

Cat. No. M3796
SB-334867 Structure
Size Price Availability
10mg USD 150 Out of stock
50mg USD 480 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SB-334867 has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. SB-334867-A is a non-peptide OX(1) selective receptor antagonist. PKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. SB-334867 blocks orexin-A induced grooming and feeding following systemic administration in vivo. SB-334867-A (OX1, pKB = 7.4; OX2, pKB = 5.7), devoid of appreciable affinity for either 5-HT2B (pKi < 5.3) or 5-HT2C (pKi < 5.4) receptors, provides the first definitive evidence that a central behavioural effect of orexin-A (grooming) is mediated by OX1 receptors.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male and female Sprague–Dawley rats
Formulation 10% (w/v) Encapsin in sterile water
Dosages 30 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 355.78
Formula C17H14ClN5O2
CAS Number 249889-64-3
Purity >99%
Solubility DMSO
Storage at -20°C
References

1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Porter RA, et al. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. PMID: 11459658.

SB-334867-A: the first selective orexin-1 receptor antagonist.
Smart D, et al. Br J Pharmacol. 2001 Mar;132(6):1179-82. PMID: 11250867.

Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement.
Duxon MS, et al. Psychopharmacology (Berl). 2001 Jan 1;153(2):203-9. PMID: 11205420.

A selective orexin-1 receptor antagonist reduces food consumption in male and female rats.
Haynes AC, et al. Regul Pept. 2000 Dec 22;96(1-2):45-51. PMID: 11102651.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB-334867 supplier, OX Receptor, inhibitors

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