中文名称: | SB-222200 | ||||
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英文名称: | SB-222200 | ||||
别名: | (S)-3-甲基-2-苯基-N-(1-苯基丙基)喹啉-4-甲酰胺 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide | ||||
CAS No: | 174635-69-9 | 分子式: | C26H24N2O | 分子量: | 380.48 |
CAS No: | 174635-69-9 | ||||
分子式: | C26H24N2O | ||||
分子量: | 380.48 |
基本信息
产品编号: |
S11188 |
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产品名称: |
SB-222200 |
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CAS: |
174635-69-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
380.48 |
-20℃ |
1个月 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.6283mL |
13.1413mL |
26.2826mL |
5mM |
0.5257mL |
2.6283mL |
5.2565mL |
10mM |
0.2628mL |
1.3141mL |
2.6283mL |
生物活性
产品描述 |
一种有效、选择性、口服活性的,具有血脑屏障 (BBB) 渗透性的 NK-3 受体 (NK-3 receptor) 拮抗剂。SB-222200 被开发用于中枢神经系统疾病的研究。 |
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靶点 |
NK3 |
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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 4.4nM.SB-222200 antagonizes NKB-induced Ca2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK3R) with an IC50 of 18.4nM.SB-222200 is selective for hNK-3 receptors compared with hNK-1 (Ki>100,000nM) and hNK-2 receptors (Ki=250nM).SB-222200 (10 nM-1μM) produces a concentration-dependent,surmountable inhibition of NKB-induced Ca2+ mobilization in HEK 293-hNK-3R cells. |
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体内研究 |
SB-222200 (5mg/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 427ng/mL) following oral administration (rat 10mg/kg).SB-2222006 exhibits terminal elimination half-life (rat 1.9h) due to high plasma clearance (56mL/min/kg) following intravenous administration (rat 2.5mg/kg). |
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Animal Model: |
Male BALB/c mice (19-21g) |
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Dosage: |
5mg/kg |
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Administration: |
Oral administration |
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Result: |
Produced 57% inhibition of senktide-induced behavioral responses in mice. |
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Animal Model: |
Male Sprague-Dawley rats (300-400g) |
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Dosage: |
2.5mg/kg for i.v.;10mg/kg for p.o.(Pharmacokinetic Analysis) |
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Administration: |
Intravenous injection and oral gavage |
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Result: |
Oral bioavailability (46%),T1/2 (1.9h),Cmax (427ng/mL). |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )