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SB-222200

    
99%

SB-222200

源葉(MedMol)
S83948 一鍵復制產品信息
174635-69-9
C26H24N2O
380.48
MFCD00944072
Lopac-S-5192; Tocris-1393;
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S83948-5mg 99% ¥510.00 6 - - -
S83948-10mg 99% ¥850.00 7 - - -
S83948-25mg 99% ¥1700.00 6 - - -
S83948-100mg 99% ¥4930.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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

產品描述: 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
靶點: NK3;Neurokininreceptor
體外研究: 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.
體內研究: 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).
參考文獻: 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
保存條件: -20℃
配置溶液濃度參考:
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
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參考文獻

質檢證書(COA)

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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

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