TPH2 agonist-1
TPH2 agonist-1 (compound 20e) is an orally active, blood-brain barrier permeable, 1,3,4-oxadiazol-2 (3H)-one-derived TPH2 agonist. TPH2 agonist-1 upregulates TPH2 expression, elevates 5-HT and GABA levels, and exhibits antiepileptic activity in SCN1A-deficient models. TPH2 agonist-1 stabilizes the electrophysiological activity of neuronal networks and inhibits abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity, and it can be used in studies related to severe myoclonic epilepsy of infancy (Dravet syndrome).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C15H8ClF4N3O2
- Molecular Weight:373.69
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
In Vitro
TPH2 agonist-1 (compound 20e) dose-dependently inhibits the abnormal electrophysiological activity of iPSC-derived neurons from SMEI patients. At 1 μM, it significantly reduces the average firing rate and burst percentage, while at 10 μM and 50 μM, it further decreases the network burst frequency and duration[1].
Treatment of wild-type (WT) and scn1lab KO zebrafish larvae with TPH2 agonist-1 (5 μM; 4 h) increases the levels of serotonin (5-HT) and γ-aminobutyric acid (GABA), and restores 5-HT immunoreactivity in the hypothalamus of KO larvae[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VERO, HFL-1, L929, NIH3T3, CHO-K1
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
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Incubation Time:24 h
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Result:Did not affect the viability of various mammalian cell lines, with an IC50 value greater than 100 μM in all tested cell lines as determined by WST analysis.
In Vivo
TPH2 agonist-1 (5 mg/kg; administered via oral gavage; single dose; heat induction performed 30 min post-administration) significantly reduces seizure severity, prolongs the latency to the first seizure, increases the seizure threshold temperature, and inhibits hyperactivity in SCN1A+/- mice, with no effect on the behaviors of wild-type mice[1].
TPH2 agonist-1 (2.5 μM, 5 μM; waterborne exposure; single exposure; recording performed 30 min post-exposure) dose-dependently reduces seizure-like locomotion in scn1lab KO zebrafish larvae, with a 41.58% reduction at 2.5 μM and a 16.3% reduction at 5 μM. It does not affect the normal locomotion of wild-type zebrafish and can also restore the blue color preference of KO larvae[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:13-15-week-old male and female 129S-Scn1atm1Kea/Mmjax heterozygous mice (SCN1A+/-) and WT littermates + SMEI model[1]
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Dosage:5 mg/kg
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Administration:gavage; frequency: single dose; 30 min before heat induction
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Result:Significantly reduced seizure severity in SCN1A+/- mice, decreasing the Racine scale score by 52% compared with vehicle control, prolonged the latency to the first seizure, and increased the seizure threshold temperature. It also suppressed hyperactivity in SCN1A+/- mice by reducing total distance traveled and average speed, without affecting the locomotor behavior of WT mice.
Chemical Information
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Molecular Weight 373.69
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Formel C15H8ClF4N3O2
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SMILES
FC(C=C1)=CC(Cl)=C1CN2C(OC(C3=CC(C(F)(F)F)=NC=C3)=N2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
TPH2 agonist-1 Related Classifications
HY-181575 Related Classifications
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