SB-222200

SKU: orb1218629

Description

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

Key Properties

• CAS Number: 174635-69-9
• MW: 380.48
• Purity: >98% (HPLC)
• 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
• Target: Neurokinin Receptor
• Solubility: DMSO:100 mg/mL (262.83 mM)

Bioactivity

• In Vivo:
  SB-222200 (5 mg/kg; 30 min pretreatment) produces inhibition of behavioral responses induced by NK-3 receptor-selective agonist senktide (HY-P0187) in mice. SB-2222006 exhibits moderate oral bioavailability (rat 46%) and Cmax (rat 427 ng/mL) following oral administration (rat 10 mg/kg). SB-2222006 exhibits terminal elimination half-life (rat 1.9 h) due to high plasma clearance (56 mL/min/kg) following intravenous administration (rat 2.5 mg/kg). Animal model: Male BALB/c mice (19-21 g). Dosage: 5 mg/kg. Administration: Oral administration. Result: Produced 57% inhibition of senktide-induced behavioral responses in mice. Animal model: Male Sprague-Dawley rats (300-400 g). Dosage: 2.5 mg/kg for i. v. ; 10 mg/kg for p.o. (Pharmacokinetic Analysis). Administration: Intravenous injection and oral gavage. Result: Oral bioavailability (46%), T1/2 (1.9 h), Cmax (427 ng/mL).
• In Vitro:
  SB-222200 inhibits 125I-[MePhe7]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a Ki of 4.4 nM. SB-222200 antagonizes NKB-induced Ca2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC50 of 18.4 nM. SB-222200 is selective for hNK-3 receptors compared with hNK-1 (Ki>100, 000 nM) and hNK-2 receptors (Ki=250 nM). SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca2+ mobilization in HEK 293-hNK-3R cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Neurokinin Receptor