SB-222200
(Synonyms: 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺,SB 222200;SB222200) 目录号 : GC10107
An NK3 receptor antagonist
Cas No.:174635-69-9
Sample solution is provided at 25 µL, 10mM.
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SB 222200 is a selective and potent antagonist of NK-3 receptor [1].
Neurokinin-3 (NK-3) receptor is a member of the G-protein-coupled superfamily and functions as a receptor for tachykinin. Activation of NK-3 receptors causes phosphoinositol 4, 5 biphosphate
(PIP2) breakdown into 1,4,5 inositol triphosphate (IP3) and diacylglycerol through phospholipase C activation [1].
In Chinese hamster ovary (CHO) cell expressing the hNK-3 receptor, SB 222200 inhibited neurokinin B (NKB) binding to the cell membranes with a Ki value of 4.4 nM. In HEK 293 cells expressing the hNK-3 receptor, SB 222200 antagonized NKB-induced Ca2+ mobilization with an IC50 value of 18.4 nM [1].
In mice model, SB-222200 inhibited behavioral responses (rapid head shakes and tail whips) induced by senktide (the NK-3 receptor-selective agonist) with an ED50 value of 5 mg/kg in a dose-dependent way and the inhibitory effect correlated significantly with brain concentrations of SB-222200 [1]. Treatment adult male CD-1 mice with SB 222200, mice had significantly enhanced hyperactivity when challenged with cocaine, which suggested that blockade of NK-3 receptors enhanced dopamine-mediated behavioral hyperactivity.
References:
[1]. Sarau HM, Griswold DE, Bush B, 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, 295(1): 373-381.
[2]. Nwaneshiudu CA, Unterwald EM. Blockade of neurokinin-3 receptors modulates dopamine-mediated behavioral hyperactivity. Neuropharmacology, 2009, 57(3): 295-301.
| Cas No. | 174635-69-9 | SDF | |
| 别名 | 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺,SB 222200;SB222200 | ||
| 化学名 | 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide | ||
| Canonical SMILES | CCC(C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)C | ||
| 分子式 | C26H24N2O | 分子量 | 380.48 |
| 溶解度 | ≥ 19.024 mg/mL in DMSO, ≥ 43.6 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet