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| 25mg |
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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.
| Targets |
sigma-1 receptor ( IC50 = 0.86 μM ); muscarinic
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| 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].
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| ln Vivo |
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| 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.
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| References |
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| Additional Infomation |
See also: Blarcamesine (annotation moved to).
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| Molecular Formula |
C19H24CLNO
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|---|---|
| Molecular Weight |
317.857
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| Exact Mass |
317.154
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| Elemental Analysis |
C, 71.80; H, 7.61; Cl, 11.15; N, 4.41; O, 5.03
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| CAS # |
195615-84-0
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| Related CAS # |
Blarcamesine; 195615-83-9; 195615-84-0 (HCl)
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| PubChem CID |
46932299
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
298
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O1C([H])([H])C([H])([H])C([H])(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C1(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
FEQOLYDPQKHFTD-UHFFFAOYSA-N
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| 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
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| Chemical Name |
1-(2,2-diphenyloxolan-3-yl)-N,N-dimethylmethanamine;hydrochloride
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| Synonyms |
Anavex2-73; Anavex 2-73; Anavex-2-73; Anavex-273; AE-37 hydrochloride; Anavex273; Anavex 273
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~64 mg/mL (78.7~201.4 mM)
Water: ~64 mg/mL Ethanol: ~3 mg/mL |
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| 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. View More
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. 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. |
| 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.
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.
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