| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Frovatriptan succinate hydrate, the succinate and hydrated form of frovatriptan, is a novel and potent 5-HT1B, HT1D receptor agonist and 5-HT7 receptor agonist. Frovatriptan succinate binds selectively and with high affinity to 5-HT 1B and presynaptic 5-HT 1D receptors in the extracerebral and intracranial arteries. This leads to an inhibition of serotonin activity and results in vasoconstriction of the painfully dilated blood vessels during migraine attack. Frovatriptan succinate is indicated for the acute treatment of migraine.
| Targets |
|
|
|---|---|---|
| ln Vitro |
Migraine pathophysiology is thought to be primarily driven by neurogenic inflammation and cerebral vasodilatation. Brain vasodilatation is reversed by 5-HT1B activation, while neurogenic inflammation is avoided by 5-HT1D activation. 5-HT1B and 5-HT1D receptors are highly affinified for frovatriptan, whereas 5-HT1A and 5-HT1F receptor subtypes are only moderately affinized for the drug. Dog coronary artery relaxation is linked to frovatriptan's modest affinity for 5-HT7 receptors[1].
|
|
| ln Vivo |
Frovatriptan has an oral bioavailability of 22%–30%, which is unaffected by meals. 60%–70% of the plasma's maximal concentration is reached in an hour, even though it takes two to three hours to reach its maximum. It takes four to five days to reach a stable condition. The binding of plasma proteins is just 15%. The relative terminal long half-life of roughly 26 hours is the most distinctive trait. Since frovatriptan is mostly metabolized by CYP1A2 and excreted by the kidney and liver, mild failure of either organ should not be a treatment-limiting factor[1]. When dogs are treated with frovatriptan (0.1, 0.2, and 0.3 mg/kg; administered as a single bolus intraduodenal injection), their carotid vascular resistance increases and remains elevated for at least five hours[2].
|
|
| References |
[1]. Kelman L. Review of frovatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2008 Feb;4(1):49-54.
[2]. Comer MB. Et al. Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53. |
| Molecular Formula |
C18H25N3O6
|
|---|---|
| Molecular Weight |
379.40800
|
| CAS # |
158930-17-7
|
| Related CAS # |
Frovatriptan;158747-02-5;Frovatriptan succinate;158930-09-7
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
CN[C@@H]1CCC2=C(C3=CC(C(=O)N)=CC=C3N2)C1
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~263.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
