2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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AVN-211

AVN-211 Chemical Structure

CAS No. : 1173103-84-8

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AVN-211 Related Antibodies

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Description

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[1].

IC50 & Target[1]

5-HT6 Receptor

2.34 nM (IC50)

In Vitro

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.

AVN-211 Related Antibodies
Parmacokinetics
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
In Vivo

AVN-211 (0.05-1 mg/kg, i.p. or 0.2 mg/kg, p.o., single dose) significantly reverses memory impairment, and its effect is superior to that of Memantine (HY-B0591) (5 mg/kg) and Tacrine (10 mg/kg) (HY-111338) in mice[1].
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.
Molecular Weight

333.43

Formula

C15H15N3O2S2
CAS No.
SMILES

O=S(C1=C2N=C(C)C=C(C)N2N=C1SC)(C3=CC=CC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AVN-211 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AVN-2111173103-84-8AVN211AVN 2115-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT6RantagonistsAlzheimer’s diseaseselectivitypreclinical studypharmacokineticsInhibitorinhibitorinhibit

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