货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T28527-1ml	10mM in DMSO	￥460.00 T28527-1ml ￥460.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T28527-1ml

10mM in DMSO

￥460.00

货期：3-5天

产品描述：

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

靶点：

NK3

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.

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).

参考文献：

1. 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.

溶解性：

soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.628 ml	13.141 ml	26.283 ml
5 mM	0.526 ml	2.628 ml	5.257 ml
10 mM	0.263 ml	1.314 ml	2.628 ml
50 mM	0.053 ml	0.263 ml	0.526 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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