SB-222200

Research use only, not for human use.

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

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

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.

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).

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GPCR/G Protein

Neurokinin Receptor

NK3

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174635-69-9

380.48

C26H24N2O

>98% (HPLC)

DMSO:100 mg/mL (262.83 mM)

O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC

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(-20℃)

With Ice Pack

≥ 2 years