| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
H1 Receptor mGluR 1 84 nM (Ki) mGluR2 1.65 μM (Ki)
M1 muscarinic receptor (high affinity, Ki = 84 nM) and M2 muscarinic receptor (low affinity, Ki = 1.65 μM). Also acts as a histamine H1 receptor blocker. |
|---|---|
| ln Vitro |
Oxomemazine is a selective M1 receptor antagonist with a Ki of 84 nM for the M1 receptor and 1.65 μM for the M2 receptor. It displays about a 20-fold difference in affinity between the two receptor subtypes. It also acts as a histamine H1 receptor blocker.
|
| ln Vivo |
No detailed in vivo activity data are publicly available for oxomemazine. As an M1-selective antagonist and H1 blocker, its in vivo effects would be expected to be related to modulation of cholinergic and histaminergic neurotransmission.
|
| Enzyme Assay |
In vitro receptor binding assays for oxomemazine are performed to evaluate its affinity for M1 and M2 muscarinic receptors and H1 receptors. Radioligand binding studies using membrane preparations from cells or tissues expressing the target receptors are conducted. The compound's ability to displace specific radiolabeled ligands is measured to calculate its Ki values.
|
| Cell Assay |
In vitro cell-based assays are conducted using cells expressing M1 or M2 muscarinic receptors. The cells are treated with oxomemazine, and receptor antagonism is measured by assessing its ability to block agonist-induced downstream signaling events such as calcium mobilization or PI hydrolysis.
|
| Animal Protocol |
In vivo animal studies would be conducted in rodent models to evaluate the effects of oxomemazine on cough and cholinergic neurotransmission. The compound could be administered via various routes, and its effects on cough reflex and other behaviors could be assessed.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for oxomemazine. As a research compound, its ADME properties would be characterized in standard preclinical studies.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for oxomemazine. As an M1 receptor antagonist and H1 blocker, its toxicity profile is expected to be related to its mechanism of action.
|
| References | |
| Additional Infomation |
Oxomemazine belongs to the phenothiazine class of compounds.
Oxomemazine is a selective M1 receptor antagonist (Ki = 84 nM) with about 20-fold selectivity over the M2 receptor (Ki = 1.65 μM). It also acts as a histamine H1 receptor blocker. The compound is used in cough-related research and is not approved for human therapeutic use. |
| 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
|
| SMILES |
CC(CN1C2=CC=CC=C2S(=O)(=O)C3=CC=CC=C31)CN(C)C
|
| 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)
|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (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.
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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