TGF-8027
TGF-8027 is a selective 5-HT2A receptor agonist with a Ki of 7.4 nM and an EC50 of 3.3 nM at the human receptor. TGF-8027 activates the 5-HT2A receptor-mediated Gq protein signaling pathway. TGF-8027 induces dose-dependent head-twitch responses in mice.
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- CAS No.: 3136748-24-5
- Formule: C19H22N2O3
- Masse moléculaire:326.39
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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
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Activité biologique
Description
IC50 & Target
[1]|
5-HT2A Receptor 7.4 nM (Ki) |
5-HT2A Receptor 3.3 nM (EC50) |
In Vitro
TGF-8027 (60 minutes at 37°C) shows 368-fold selectivity for 5-HT2A over 5-HT2C VGV in the Gq dissociation BRET assay in HEK293T cells[1].
TGF-8027 (60 minutes at 37°C) has an EC50 of 14 nM for mouse 5-HT2A in HEK293T cells and shows reduced selectivity for mouse 5-HT2C[1].
TGF-8027 exhibits 85-fold selectivity for 5-HT2A over 5-HT2C in calcium flux assays in Flp-In 293 T-Rex cells[1].
TGF-8027 (60 minutes at 37°C) recruits β-arrestin2 at 5-HT2A in HEK293T cells with an EC50 of 4.5 nM and an Emax of 108%[1].
TGF-8027 binds to human 5-HT2A with an affinity of 7.4 nM and exhibits 149-fold selectivity for 5-HT2A over 5-HT2C in a cell-free radioligand binding assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks old)[1]
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Dosage:5 mL/kg
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Administration:s.c.; single injection per test session; 30-minute recording period
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Result:The ED50 was 1.86 mg/kg (95% CI 1.18-2.92).
Chemical Information
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CAS No. 3136748-24-5
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Masse moléculaire 326.39
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Formule C19H22N2O3
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SMILES
COC1=C(CCNC(C)C2=CC=CC=C2O)C=C(OC)C(C#N)=C1
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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)
TGF-8027 Related Classifications
HY-178760 Related Classifications
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