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Tasipimidine sulfate 1465908-73-9

Tasipimidine sulfate 1465908-73-9

CAS No.: 1465908-73-9

Tasipimidine sulfate is an orally bioactive, selective α2A-adrenoceptor agonist with pEC50 of 7.57 for human α2A-adren
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

Tasipimidine sulfate is an orally bioactive, selective α2A-adrenoceptor agonist with pEC50 of 7.57 for human α2A-adrenoceptor. Tasipimidine sulfate may be utilized in the research/study of situational anxiety and fear.

Physicochemical Properties


Molecular Formula C13H18N2O6S
Molecular Weight 330.36
Exact Mass 330.088
CAS # 1465908-73-9
PubChem CID 89851688
Appearance White to off-white solid powder
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 2
Heavy Atom Count 22
Complexity 387
Defined Atom Stereocenter Count 0
SMILES

S(O)(O)(=O)=O.O(C1C=CC=C2C(C3=NCCN3)OCCC=12)C

InChi Key HZWPSPYSMWTZTG-UHFFFAOYSA-N
InChi Code

InChI=1S/C13H16N2O2.H2O4S/c1-16-11-4-2-3-10-9(11)5-8-17-12(10)13-14-6-7-15-13;1-5(2,3)4/h2-4,12H,5-8H2,1H3,(H,14,15);(H2,1,2,3,4)
Chemical Name

2-(5-methoxy-3,4-dihydro-1H-isochromen-1-yl)-4,5-dihydro-1H-imidazole;sulfuric acid
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

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)

Biological Activity


References

[1]. Tasipimidine-the pharmacological profile of a novel orally active selective α2A-adrenoceptor agonist. Eur J Pharmacol. 2022 May 15;923:174949.

Additional Infomation Drug Indication
Alleviation of situational anxiety and fear in dogs triggered by e. g. travel, noise, owner departure, veterinary visits.

Solubility Data


Solubility (In Vitro) DMSO : ~125 mg/mL (~378.38 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.08 mg/mL (6.30 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 20.8 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: ≥ 2.08 mg/mL (6.30 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 20.8 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.

Solubility in Formulation 3: ≥ 2.08 mg/mL (6.30 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0270 mL 15.1350 mL 30.2700 mL
5 mM 0.6054 mL 3.0270 mL 6.0540 mL
10 mM 0.3027 mL 1.5135 mL 3.0270 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.