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Frovatriptan (succinate hydrate)

Katalog-Nr.GC45458

 

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Frovatriptan (succinate hydrate) Chemische Struktur

Cas No.: 158930-17-7

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Sample solution is provided at 25 µL, 10mM.

Description of Frovatriptan (succinate hydrate)

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.

References
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 receptors. Br. J. Pharmacol. 119(Suppl 1), 110P (1996).
2. Comer, M.B. Pharmacology of the selective 5-HT1B/1D agonist frovatriptan. Headache 42(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 arteries. J. 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 dogs. J. Cardiovasc. Pharmacol. 30(1), 136-141 (1997).

Chemical Properties of Frovatriptan (succinate hydrate)

Cas No. 158930-17-7 SDF
Canonical SMILES O=C(N)C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1.OC(CCC(O)=O)=O.O
Formula C14H17N3O.C4H6O4[H2O] M.Wt 379.4
Löslichkeit DMF: 3mg/mL,DMSO: 10mg/mL,PBS (pH 7.2): 5mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Frovatriptan (succinate hydrate)

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6357 mL 13.1787 mL 26.3574 mL
5 mM 527.1 μL 2.6357 mL 5.2715 mL
10 mM 263.6 μL 1.3179 mL 2.6357 mL
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In vivo Formulation Calculator (Clear solution) of Frovatriptan (succinate hydrate)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 7 reference(s) in Google Scholar.)

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