产品
编 号：F209426
分子式：C26H24N2O
分子量：380.48
分子式：C26H24N2O
分子量：380.48
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规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 174635-69-9
产品详情
生物活性：
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
体内研究：
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).
体外研究：
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 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
体内研究：
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).
体外研究：
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.
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