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Oxomemazine 3689-50-7

Oxomemazine 3689-50-7

CAS No.: 3689-50-7

Oxomemazine is a phenothiazine-based histamine H1-receptor antagonist (blocker) with significant antimuscarinic activity
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This product is for research use only, not for human use. We do not sell to patients.

Oxomemazine is a phenothiazine-based histamine H1-receptor antagonist (blocker) with significant antimuscarinic activity. Oxomemazine is a selective antagonist of the histamine M1 receptor, exhibiting both high (histamine H1-receptor=84 nM, M1 receptor) and low (histamine H1-receptor=1.65 μM, M2 receptor) affinity sites. 20x difference. Oxomemazine is an antihistamine and anticholinergic agent used in research related to cough research.

Physicochemical Properties


Molecular Formula C18H22N2O2S
Molecular Weight 330.44
Exact Mass 330.14
CAS # 3689-50-7
PubChem CID 19396
Appearance White to off-white solid powder
Density 1.2±0.1 g/cm3
Boiling Point 492.4±34.0 °C at 760 mmHg
Flash Point 251.6±25.7 °C
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.598
LogP 2.85
Hydrogen Bond Donor Count 0
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 4
Heavy Atom Count 23
Complexity 470
Defined Atom Stereocenter Count 0
InChi Key QTQPVLDZQVPLGV-UHFFFAOYSA-N
InChi Code

InChI=1S/C18H22N2O2S/c1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)23(21,22)18-11-7-5-9-16(18)20/h4-11,14H,12-13H2,1-3H3
Chemical Name

3-(5,5-dioxophenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
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)

Biological Activity


Targets H1 Receptor mGluR 1 84 nM (Ki) mGluR2 1.65 μM (Ki)
References

[1]. Selectivity of oxomemazine for the M1 muscarinic receptors.Arch Pharm Res. 1994 Dec;17(6):443-51.

[2]. Oxomemazine hydro-chloride. Acta Crystallogr Sect E Struct Rep Online. 2011 Aug 1;67(Pt 8):o1875.

Additional Infomation Oxomemazine is a member of phenothiazines.

Solubility Data


Solubility (In Vitro) DMSO: 100 mg/mL (302.63 mM)
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0263 mL 15.1313 mL 30.2627 mL
5 mM 0.6053 mL 3.0263 mL 6.0525 mL
10 mM 0.3026 mL 1.5131 mL 3.0263 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.