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製品番号: HY-B1658B

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Frovatriptan succinate

(別名: (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate)

Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 158930-09-7
分子式: C₁₈H₂₃N₃O₅
分子量:361.39

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

Frovatriptan succinate 構造式

CAS 番号: 158930-09-7

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
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関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[2]

5-HT_1A Receptor

5-HT_1B Receptor

5-HT_1F Receptor

5-HT₇ Receptor

5-HT_1B Receptor

8.2 (pEC₅₀)

5-HT_1D Receptor

5-HT Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT_1B reverses cerebral vasodilatation and activation of 5-HT_1D prevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT_1B and 5-HT_1D receptors and a moderate affinity for the 5-HT_1A and 5-HT_1F receptors subtypes. Frovatriptan has a moderate affinity for the 5-HT₇ receptors, an action associated with coronary artery relaxation in the dog^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Oral bioavailability of Frovatriptan is 22%-30% and is not affected by food. Although the maximum concentration in the plasma is achieved in 2-3 hours, 60%-70% of this is achieved in 1 hour. A steady state is achieved in 4-5 days. Plasma protein binding is low at 15%. The most unique feature is the relative terminal long half-life of about 26 hours. Frovatriptan is chiefly metabolized by CYP1A2 and is cleared by the kidney and liver making moderate failure of either organ not a limiting factor in treatment^[1].
Frovatriptan (0.1, 0.2, and 0.3 mg/kg; a single bolus intraduodenal administration) treatment produces an increase in carotid vascular resistance, which is sustained for at least 5 hours in dogs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 158930-09-7
分子量 361.39
分子式 C₁₈H₂₃N₃O₅
SMILES

O=C(O)CCC(O)=O.O=C(C1=CC2=C(NC3=C2C[C@H](NC)CC3)C=C1)N
別名

(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Kelman L. Review of frovatriptan in the treatment of migraine. Neuropsychiatr Dis Treat. 2008 Feb;4(1):49-54. [Content Brief]

[2]. Comer MB. Et al. Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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生物活性
- 製品説明
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- 体内実験
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参考文献

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Frovatriptan succinate

5-HT Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Frovatriptan succinate 関連分類

HY-B1658B 関連分類