Anavex2-73 HCl

Alias: Anavex2-73; Anavex 2-73; Anavex-2-73; Anavex-273; AE-37 hydrochloride; Anavex273; Anavex 273
Cat No.:V7110 Purity: ≥98%
Anavex2-73 (Anavex-273; AE-37) HCl is a novel and potent muscarinic/σ1 ( Sigma-1) ligand/agonist (IC50 = 860 nM) with therapeutic potential for treating Alzheimer's disease.
Anavex2-73 HCl Chemical Structure CAS No.: 195615-84-0
Product category: Sigma Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Anavex2-73 HCl:

  • Blarcamesine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description

Anavex2-73 (Anavex-273; AE-37) HCl is a novel and potent muscarinic/σ1 ( Sigma-1) ligand/agonist (IC50 = 860 nM) with therapeutic potential for treating Alzheimer's disease.

Biological Activity I Assay Protocols (From Reference)
Targets
sigma-1 receptor ( IC50 = 0.86 μM ); muscarinic
ln Vitro
The pre-administration of AVex-73 hydrochloride (ANAVEX2-73) leads to a dose-dependent attenuation of the scopolamine induced alternation deficit, significant at 1 and 3 mg/kg. The step-through latency impairments are significantly reduced, dose-dependently, at doses greater than 0.3 mg/kg, by pre-treating with AVex-73 hydrochloride[1]. Significant improvement in recognition memory deficit is observed at 1 mg/kg of AVex-73 hydrochloride treatment, which is administered in a dose-dependent manner. AVex-73 hydrochloride, at doses of 0.1 and 1 mg/kg, significantly attenuates the significant Aβ25-35-induced decrease in Akt phosphorylation one day after injections. The reduction in Ser9 phosphorylation caused by the peptide at 0.3 and 1 mg/kg is lessened seven days after injections by AVex-73 hydrochloride. The administration of AVex-73 hydrochloride treatment inhibits the rise in Aβ1-42 content induced by Aβ25-35 in a dose-dependent manner, exhibiting a noteworthy impact at the maximum dosage examined[2].
ln Vivo
The pre-administration of AVex-73 hydrochloride (ANAVEX2-73) leads to a dose-dependent attenuation of the scopolamine induced alternation deficit, significant at 1 and 3 mg/kg. The pre-treatment with AVex-73 hydrochloride attenuates the impairments of step-through latency, dose dependently and significantly at doses higher than 0.3 mg/kg[1]. The AVex-73 hydrochloride treatment dose-dependently blocks the recognition memory deficit, with a significant effect measured at 1 mg/kg. One day after injections, the significant Aβ25-35-induced decrease in Akt phosphorylation is significantly attenuated by AVex-73 hydrochloride at 0.1 and 1 mg/kg dose. Seven days after injections,AVex-73 hydrochloride attenuates the decrease in Ser9 phosphorylation induced by the peptide at 0.3 and 1 mg/kg. The AVex-73 hydrochloride treatment dose-dependently prevents the Aβ25-35-induced increase in Aβ1-42 content, with a significant effect at the highest dose tested[2].
Animal Protocol
We use male mice that weigh 32±2 g and are 7–9 weeks old. Substances, such as brahmenesine hydrochloride, are diluted to the appropriate dose and injected at a 100 μL/20 g body weight volume. Animals are used for behavioral testing from day 1 to day 9 following intravenous injections, or they are killed prior to biochemical measures.
References

[1]. J Psychopharmacol . 2011 Aug;25(8):1101-17.

[2]. Neuropsychopharmacology . 2013 Aug;38(9):1706-23.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H24CLNO
Molecular Weight
317.857
Exact Mass
317.15
Elemental Analysis
C, 71.80; H, 7.61; Cl, 11.15; N, 4.41; O, 5.03
CAS #
195615-84-0
Related CAS #
Blarcamesine; 195615-83-9; 195615-84-0 (HCl)
Appearance
Solid powder
SMILES
CN(C)CC1CCOC1(C2=CC=CC=C2)C3=CC=CC=C3.Cl
InChi Key
FEQOLYDPQKHFTD-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H23NO.ClH/c1-20(2)15-18-13-14-21-19(18,16-9-5-3-6-10-16)17-11-7-4-8-12-17;/h3-12,18H,13-15H2,1-2H3;1H
Chemical Name
1-(2,2-diphenyloxolan-3-yl)-N,N-dimethylmethanamine;hydrochloride
Synonyms
Anavex2-73; Anavex 2-73; Anavex-2-73; Anavex-273; AE-37 hydrochloride; Anavex273; Anavex 273
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25~64 mg/mL (78.7~201.4 mM)
Water: ~64 mg/mL
Ethanol: ~3 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (7.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 100 mg/mL (314.61 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1460 mL 15.7302 mL 31.4604 mL
5 mM 0.6292 mL 3.1460 mL 6.2921 mL
10 mM 0.3146 mL 1.5730 mL 3.1460 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Effect of (a, b) ANAVEX2-73, (c, d) PRE-084, and (e, f) xanomeline in the novel object recognition procedure in Aβ25–35-treated mice: (a, c, e) day 1 session, (b, d, f) day 2 session. Neuropsychopharmacology . 2013 Aug;38(9):1706-23.
  • Effect of ANAVEX2-73 (a, d), PRE-084 (b, e), and xanomeline (c, f) on GSK-3β phosphorylation in the hippocampus, 7 days after Aβ25–35 injection in mice. Neuropsychopharmacology . 2013 Aug;38(9):1706-23.
  • Effect of ANAVEX2-73 (a, b), PRE-084 (c, d), and xanomeline (e, f) on hyper- and abnormal phosphorylation of Tau protein in the hippocampus, 7 days after Aβ25–35 injection in mice. Neuropsychopharmacology . 2013 Aug;38(9):1706-23.
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