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Ethopropazine Hydrochloride 1094-08-2

Ethopropazine Hydrochloride 1094-08-2

CAS No.: 1094-08-2

Ethopropazine (Isothazine) HCl is a potent and specific inhibitor of BChE and a poor inhibitor of AChE. Ethopropazine (I
Data collection:peptidedb@qq.com

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

Ethopropazine (Isothazine) HCl is a potent and specific inhibitor of BChE and a poor inhibitor of AChE. Ethopropazine (Isothazine) HCl is a phenothiazine compound with anticholinergic properties that may be used in Parkinson's disease (PD) research.

Physicochemical Properties


Molecular Formula C19H25CLN2S
Molecular Weight 348.93
Exact Mass 348.143
CAS # 1094-08-2
Related CAS # 1094-08-2 (HCl);522-00-9;
PubChem CID 122824
Appearance White to off-white solid powder
Boiling Point 430.1ºC at 760 mmHg
Melting Point 225 - 228 °C
Flash Point 213.9ºC
Vapour Pressure 1.34E-07mmHg at 25°C
LogP 5.886
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 5
Heavy Atom Count 23
Complexity 322
Defined Atom Stereocenter Count 0
InChi Key VXPCQISYVPFYRK-UHFFFAOYSA-N
InChi Code

InChI=1S/C19H24N2S.ClH/c1-4-20(5-2)15(3)14-21-16-10-6-8-12-18(16)22-19-13-9-7-11-17(19)21;/h6-13,15H,4-5,14H2,1-3H3;1H
Chemical Name

N,N-diethyl-1-phenothiazin-10-ylpropan-2-amine;hydrochloride
Synonyms

Ethopropazine Hydrochloride; Pardisol; Dibutil; Parphezein; Profenamine HCl Parfezin;
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 (e.g. under nitrogen), avoid exposure to moisture and light.
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]. Enhancement of dissolution of ethopropazine using solid dispersions prepared with phospholipid and/or polyethylene glycol. Drug Dev Ind Pharm. 2001 May;27(5):413-8.

[2]. Activity of cholinesterases in human whole blood measured with acetylthiocholine as substrate and ethopropazine as selective inhibitor of plasma butyrylcholinesterase. Arh Hig Rada Toksikol. 2004 Apr;55(1):1-4.

Additional Infomation Profenamine hydrochloride is the monohydrochloride salt of profenamine. An antimuscarinic, it is used for the symptomatic treatment of Parkinson's disease. It has a role as an adrenergic antagonist, a histamine antagonist, an antiparkinson drug and a muscarinic antagonist. It contains a profenamine.

Solubility Data


Solubility (In Vitro) DMSO : ~25 mg/mL (~71.65 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (7.16 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 (7.16 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.

Solubility in Formulation 3: ≥ 2.5 mg/mL (7.16 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8659 mL 14.3295 mL 28.6590 mL
5 mM 0.5732 mL 2.8659 mL 5.7318 mL
10 mM 0.2866 mL 1.4330 mL 2.8659 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.