2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. 5-HT Receptor Histamine Receptor Adrenergic Receptor
  4. AVN-101 hydrochloride

AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis.

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AVN-101 hydrochloride Chemical Structure

AVN-101 hydrochloride Chemical Structure

CAS No. : 1061354-48-0

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Based on 1 publication(s) in Google Scholar

AVN-101 hydrochloride Related Antibodies

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Description

AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis[1].

IC50 & Target[1]

5-HT7 Receptor

0.153 nM (Ki)

5-HT2C Receptor

1.17 nM (Ki)

5-HT2A Receptor

1.56 nM (Ki)

5-HT6 Receptor

2.04 nM (Ki)

5-HT2B Receptor

10.6 nM (Ki)

5-HT1A Receptor

61 nM (Ki)

5-HT1B Receptor

720 nM (Ki)

H1 Receptor

0.58 nM (Ki)

Alpha-2B adrenergic receptor

0.41 nM (Ki)

Alpha-2A adrenergic receptor

1.77 nM (Ki)

Alpha-2C adrenergic receptor

3.55 nM (Ki)

Alpha-1B adrenergic receptor

9.4 nM (Ki)

Alpha-1A adrenergic receptor

18.9 nM (Ki)

Alpha-1D adrenergic receptor

30.2 nM (Ki)

Molecular Weight

340.89

Formula

C21H25ClN2
CAS No.
Unlabeled Cas

Appearance

Solid

Color

White to light yellow

SMILES

CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CC=CC=C4.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (366.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9335 mL 14.6675 mL 29.3350 mL
5 mM 0.5867 mL 2.9335 mL 5.8670 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9335 mL 14.6675 mL 29.3350 mL 73.3374 mL
5 mM 0.5867 mL 2.9335 mL 5.8670 mL 14.6675 mL
10 mM 0.2933 mL 1.4667 mL 2.9335 mL 7.3337 mL
15 mM 0.1956 mL 0.9778 mL 1.9557 mL 4.8892 mL
20 mM 0.1467 mL 0.7334 mL 1.4667 mL 3.6669 mL
25 mM 0.1173 mL 0.5867 mL 1.1734 mL 2.9335 mL
30 mM 0.0978 mL 0.4889 mL 0.9778 mL 2.4446 mL
40 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8334 mL
50 mM 0.0587 mL 0.2933 mL 0.5867 mL 1.4667 mL
60 mM 0.0489 mL 0.2445 mL 0.4889 mL 1.2223 mL
80 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
100 mM 0.0293 mL 0.1467 mL 0.2933 mL 0.7334 mL
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AVN-101 hydrochloride Related Classifications

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  • 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-1011061354-48-0AVN101AVN 1015-HT ReceptorHistamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptoranxiolytic and anti-depressive activitiescentral nervous system (CNS) diseases5-HT7 receptorhistamine H1brain-penetrantorally activeInhibitorinhibitorinhibit

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