Frovatriptan succinate hydrate
(Synonyms: 罗曲普坦琥珀酸盐,(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate) 目录号 : GC38781An agonist of 5-HT1B and 5-HT1D receptors
Cas No.:158930-17-7
Sample solution is provided at 25 µL, 10mM.
Frovatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 2.51 and 3.98 nM, respectively).1,2 It is selective for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2C, 5-HT3, and 5-HT7 receptors, as well as dopamine D1, D2, and D3, histamine H1, and α1-adrenergic receptors (Kis = >50 nM). Frovatriptan induces contractions in human basilar arteries isolated post-mortem, coronary arteries from transplant recipient hearts, and coronary arteries from donor hearts unsuitable for transplantation (EC50s = 13.8, 41.69, and 15.49 nM, respectively).3 It increases carotid vascular resistance in closed-chest and open-chest anesthetized dogs (ED50s = 6 and 1 nmol/kg, i.v., respectively).4 Formulations containing frovatriptan have been used in the treatment of migraines.
1.Brown, A.M., Parsons, A.A., Raval, P., et al.SB 209509 (VML 251), a potent constrictor of rabbit basilar artery with high affinity and selectivity for human 5-HT1D receptorsBr. J. Pharmacol.119(Suppl 1)110P(1996) 2.Comer, M.B.Pharmacology of the selective 5-HT1B/1D agonist frovatriptanHeadache42(Suppl 2)S47-S53(2002) 3.Parsons, A.A., Raval, P., Smith, S., et al.Effects of the novel high-affinity 5-HT1B/1D-receptor ligand frovatriptan in human isolated basilar and coronary arteriesJ. Cardiovasc. Pharmacol.32(2)220-224(1998) 4.Parsons, A.A., Parker, S.G., Raval, P., et al.Comparison of the cardiovascular effects of the novel 5-HT1B/1D receptor agonist, SB 209509 (VML251), and sumatriptan in dogsJ. Cardiovasc. Pharmacol.30(1)136-141(1997)
Cas No. | 158930-17-7 | SDF | |
别名 | 罗曲普坦琥珀酸盐,(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate | ||
Canonical SMILES | O=C(O)CCC(O)=O.O=C(C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1)N.O | ||
分子式 | C18H25N3O6 | 分子量 | 379.41 |
溶解度 | DMF: 3mg/mL,DMSO: 10mg/mL,PBS (pH 7.2): 5mg/mL | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6357 mL | 13.1784 mL | 26.3567 mL |
5 mM | 0.5271 mL | 2.6357 mL | 5.2713 mL |
10 mM | 0.2636 mL | 1.3178 mL | 2.6357 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
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- Purity: >99.00%
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