SB-222200, inhibitor

SB-222200

Cat. Num. AAA5755507

• Purity: 98.00%
• Synonyms: SB-222200; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (262.83mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C26H24N2O
• SMILES: O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC
• CAS Number: 174635-69-9
• Target & IC50: Others
• In Vitro: In mice, oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with the brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8mg/kg) indicated sustained plasma concentrations (C(max) = about 400ng/ml) and bioavailability of 46% [1].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for SB-222200, inhibitor

SB 222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4nM).

References

Sarau HM, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.
Sarau HM, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.