SB-222200

SKU: orb1307756

Description

SB-222200 is a potent and selective competitive antagonist of the human neurokinin-3 (NK-3) receptor, exhibiting a Ki of 4.4 nM. It is a valuable research tool for studying NK-3 receptor function in both in vitro assays and in vivo models related to reproduction, anxiety, and gastrointestinal motility.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 174635-69-9
• MW: 380.48
• Purity: 99.97%
• Formula: C₂₆H₂₄N₂O
• SMILES: C(N[C@@H](CC)C1=CC=CC=C1)(=O)C=2C3=C(N=C(C2C)C4=CC=CC=C4)C=CC=C3
• Target: Neurokinin receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.51 mM);DMSO:100 mg/mL (262.83 mM)

Bioactivity

• Target IC50:
  NK3:Ki=4.4 nM
• In Vivo:
  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 5 mg/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 (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% .
• In Vitro:
  SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, NK receptor, NK3, NK-3R, NKB, Neurokinin receptor, neurokinin-B, Neurokininreceptor, Neurokinin Receptor, nervous, central, CNS, disorders, penetrant, SB 222200, SB222200, SB-222200, system, Tachykinin receptor

Compound Identifiers

PubChem CID

9958826