AVN-211
AVN-211 (CD-008-0173) is a selective and orally active 5HT6R antagonist with an IC50 of 2.34 nM and a Ki of 1.09 nM. AVN-211 exhibits 5K-fold higher 5HT6R selectivity over other 65 receptors, enzymes, and ion channels. AVN-211 significantly improves cognitive and anxiety behaviors in various AD animal models, and has good safety profiles. AVN-211 can be used for the study of Alzheimer's dementia.
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- CAS No.: 1173103-84-8
- Formule: C15H15N3O2S2
- Masse moléculaire:333.43
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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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Activité biologique
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5-HT6 Receptor 2.34 nM (IC50) |
AVN-211 (0.1-100 μM) significantly inhibits CYP2B6 (IC50 = 0.76 μM), CYP2C9 (IC50 = 2.68 μM), and CYP2C19 (IC50 = 8.08 μM); it shows no significant inhibition on other CYP enzymes and its IC50 for the hERG potassium channel with 18 μM[1].
AVN-211 (17 μM and 500 ng/mL) exhibits high liver metabolic stability and plasma protein binding rate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Vd | Tmax | T1/2 | AUC0-t | AUC0-∞ | CL | Cmax |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 0.05 mg/kg | i.p. | 3091.39 L/kg | 5 min | 9.88 min | 197.18 min·ng/mL | 230.59 min·ng/mL | 216.83 mL/min/kg | 13.7 ng/mL |
| Mice[1] | 0.2 mg/kg | i.p. | 5381 mL/kg | 5 min | 23 min | 1205 min·ng/mL | 1259 min·ng/mL | 159 mL/min/kg | 67 ng/mL |
| Mice[1] | 1 mg/kg | i.p. | 7962 mL/kg | 5 min | 21 min | 3632 min·ng/mL | 3726 min·ng/mL | 268 mL/min/kg | 158 ng/mL |
| Monkey[1] | 10 mg/kg | p.o. | / | 15 min | 212.98 min | 12233 min·ng/mL | 14383 min·ng/mL | / | 143 ng/mL |
| Monkey[1] | 2 mg/kg | i.v. | / | 1 min | 29.34 min | 57286.3 min·ng/mL | 59571.9 min·ng/mL | / | 5732 ng/mL |
| Rat[1] | 10 mg/kg | p.o. | / | / | 131.15 min | / | 44627.8 min·ng/mL | / | 204 ng/mL |
| Rat[1] | 5 mg/kg | i.v. | / | / | 50.86 min | / | 64921.6 min·ng/mL | / | 959.7 ng/mL |
AVN-211 (0.05-0.2 mg/kg, i.p., single dose) significantly improves the navigation ability of rats, restoring the dwell time in the target quadrant to a level close to that of the control group[1].
AVN-211 (0.05-1 mg/kg, i.p., single dsose) extends the exploration time of the open arm, and its effect is comparable to that of Lorazepam, without causing motor inhibition[1].
AVN-211 (0.05-0.2 mg/kg, i.p., single dose) restores the pre-pulse inhibition (PPI) to 46-55% in mice, confirming its potential as an antipsychotic agent[1].
AVN-211 (500-20000 mg/kg, i.p., single dose or 1-400 mg/kg, p.o., for 180 days) exhibits acute toxicity LD50 of 13684 mg/kg and there is no significant weight loss or organ damage in the long-term toxicity tests, no mutagenicity is observed in mice and rats, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1173103-84-8
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Masse moléculaire 333.43
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Formule C15H15N3O2S2
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SMILES
O=S(C1=C2N=C(C)C=C(C)N2N=C1SC)(C3=CC=CC=C3)=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)
AVN-211 Related Classifications
HY-105998 Related Classifications
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