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).
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- Formule: C15H8ClF4N3O2
- Masse moléculaire:373.69
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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Masse moléculaire 373.69
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Formule 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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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)
TPH2 agonist-1 Related Classifications
HY-181575 Related Classifications
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