UCSF3384
UCSF3384 (Z1480758218) is a selective, blood-brain barrier-permeable MT1 inverse agonist, with an EC50 of 21 nM for hMT1. UCSF3384 selectively elevates basal cAMP levels. UCSF3384 delays circadian rhythm resetting and advances the onset of wheel-running activity rhythm in Mus musculus. UCSF3384 is applicable to research related to circadian rhythm disorders.
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- CAS. Nr.: 2248752-25-0
- Formel: C18H20N4
- Molecular Weight:292.38
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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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Chemical Information
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Biologische Aktivität
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MT1 21 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | EC50 |
21 nM
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Inverse agonist activity increasing basal cAMP levels in human HEK293T cells transiently expressing hMT1 receptors, measured via GloSensor cAMP biosensor assay with 15 minutes of compound incubation followed by 15 minutes of luciferin/isoproterenol incubation.
Inverse agonist activity increasing basal cAMP levels in human HEK293T cells transiently expressing hMT1 receptors, measured via GloSensor cAMP biosensor assay with 15 minutes of compound incubation followed by 15 minutes of luciferin/isoproterenol incubation.
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32040955 |
UCSF3384 exhibits higher binding affinity for the hMT1 receptor upon G protein uncoupling, with a Ki of 63 nM in the presence of GTP, confirming that it acts as an hMT1 inverse agonist[2].
UCSF3384 acts as a selective inverse agonist of hMT1 in HEK293T cells, and it increases basal cAMP levels. Its EC50 at the hMT1 receptor is 21 nM, and it shows 31-fold higher selectivity for the hMT1 receptor over the hMT2 receptor[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUC0-∞ | T1/2 | CL | Vss |
|---|---|---|---|---|---|---|---|
| Mice[2] | 2 mg/kg | i.v. | 1299.6 ng/mL | 563.8 ng·h/mL | 0.32 h | 58.48 mL/min/kg | 1.38 L/kg |
UCSF3384 (30 μg/mouse; s.c.; daily; 3 days) advances the phase of free-running circadian wheel running activity onset by an amplitude similar to melatonin when administered at subjective dusk in wild-type C3H/HeN mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeN wild-type (male and female, 3-6 months old, east-bound jet-lag model via abrupt 6-hour advance of the light-dark cycle)[2]
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Dosage:30 μg/mouse
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Administration:s.c.; daily; 3 days
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Result:Decelerated the rate of re-entrainment of running wheel activity rhythm onset to the advanced light-dark cycle.
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Animal Model:C3H/HeN wild-type (male and female, 3-8 months old, free-running circadian rhythm model in constant darkness)[2]
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Dosage:30 μg/mouse
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Administration:s.c.; daily; 3 days
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Result:Advanced the onset of running wheel activity with an amplitude similar to melatonin at this circadian time.
Chemical Information
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CAS. Nr. 2248752-25-0
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Molecular Weight 292.38
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Formel C18H20N4
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SMILES
CC(C1=CC=C(CNC2=CC=CC(C3=NC=NN3)=C2)C=C1)C
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Synonyms
Z1480758218; ZINC000157673384
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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)
UCSF3384 Related Classifications
HY-156156 Related Classifications
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