Fonagepant
Fonagepant (FE 205030) is a calcitonin gene-related peptide (CGRP) receptor antagonist with an IC50 of 0.2 nM. Fonagepant selectively blocks CGRP receptor activity, inhibits CGRP-induced vasodilation, attenuates capsaicin-induced increase in skin blood flow, and blocks CGRP-induced vasodilation in isolated human mesenteric resistance arteries. Fonagepant can be used in studies related to acute migraine attacks.
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- CAS No.: 1966181-14-5
- Formule: C66H88N16O16S2
- Masse moléculaire:1425.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.2 nM
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Inhibition of human CGRP receptor-mediated cAMP production in stably transfected HEK cells measured via time-resolved fluorescence resonance energy transfer.
Inhibition of human CGRP receptor-mediated cAMP production in stably transfected HEK cells measured via time-resolved fluorescence resonance energy transfer.
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34217775 |
In Vitro
Fonagepant (0.3-10 nM) potently blocks αCGRP-induced vasodilation of isolated human mesenteric resistance arteries, with a mean pA2 value of 9.3, and acts as a competitive antagonist[1].
Fonagepant potently inhibits cAMP production mediated by the human CGRP receptor, with an IC50 of 0.2 nM, and exhibits high selectivity for human AM1R and AM2R receptors in stably transfected HEK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male (3.0-4.0 kg)[1]
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Dosage:3 nM; 10 nM; 30 nM; 100 nM; 300 nM (target steady-state plasma concentrations)
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Administration:i.v. bolus plus infusion
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Result:Did not inhibit capsaicin-induced increases in skin blood flow relative to the control at 3 nM target steady-state plasma concentration.
Caused inhibition of capsaicin-induced skin blood flow increases beginning at 25 minutes post-capsaicin application at 10 nM target steady-state plasma concentration.
Caused inhibition of capsaicin-induced skin blood flow increases beginning at 20 minutes post-capsaicin application at 30 nM target steady-state plasma concentration.
Caused inhibition of capsaicin-induced skin blood flow increases beginning at 15 minutes post-capsaicin application at 100 nM target steady-state plasma concentration.
Caused inhibition of capsaicin-induced skin blood flow increases beginning at 25 minutes post-capsaicin application at 300 nM target steady-state plasma concentration.
Exhibited maximal inhibitory activity at circulating concentrations of 30-100 nM, where all treated animals showed decreased skin blood flow responses relative to controls.
Resulted in measured plasma concentrations within 1.4-fold of target values.
Chemical Information
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CAS No. 1966181-14-5
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Masse moléculaire 1425.63
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Formule C66H88N16O16S2
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Synonyms
FE 205030
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Sequence
{d-Val}-{Phe(CONH2)}-Cys-{Orn(1-methylethyl)}-Asp-Val-Gly-Pro-Phe-Cys-{Val(3-pyridinyl)}-NH2 (Disulfide bridge: Cys3-Cys10)
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Sequence Shortening
{d-Val}-{Phe(CONH2)}-C-{Orn(1-methylethyl)}-DVGPFC-{Val(3-pyridinyl)}-NH2 (Disulfide bridge: Cys3-Cys10)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fonagepant Related Classifications
HY-P12136 Related Classifications
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