| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Not applicable. Isopromethazine hydrochloride is a structural isomer and impurity of the H1 antihistamine promethazine. It has significantly lower affinity for the histamine H1 receptor than promethazine and is considered pharmacologically inactive. Promethazine itself acts as an antagonist of H1 receptors, as well as having anti-cholinergic and sedative effects. This impurity does not possess these activities. Its role is as a marker for the purity and stability of promethazine products.
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| ln Vitro |
In vitro, this compound is not used for biological activity studies. It is an analytical standard. In an HPLC method for promethazine, a system suitability solution is prepared containing promethazine (1 mg/mL) and the impurity at 0.1% (1 ug/mL). Using a C18 column and a mobile phase of acetonitrile:phosphate buffer (pH 2.5) (40:60), the impurity elutes with a specific relative retention time (RRT). It is used to verify the resolution of the method. It does not antagonize histamine in functional assays.
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| ln Vivo |
In vivo, this compound is not administered therapeutically. It is part of the quality control process. In stability studies of promethazine formulations, the level of this impurity is monitored to ensure product quality. It is not used in efficacy studies.
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| Enzyme Assay |
General protocol for in vitro analytical use: For HPLC analysis of Promethazine impurities, prepare mobile phase: acetonitrile: buffer (pH 2.5; 40:60). Buffer: 0.05 M KH2PO4 adjusted to pH 2.5 with H3PO4. Prepare a standard solution of Isopromethazine hydrochloride at 1 ug/mL in mobile phase. Inject 20 uL onto a C18 column (4.6 × 150 mm, 5 um) at 30degC. Flow rate: 1.0 mL/min. UV detection at 254 nm. The retention time of promethazine is ~8 min, and the impurity elutes with a RRT of ~0.9. Validate the method for specificity and linearity (0.1-5 ug/mL). The reference standard is stored at -20degC. For LC-MS, use positive mode with m/z 285 [M+H]+ (free base).
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| Cell Assay |
General protocol for in vitro cell-based experiments: Not applicable for biological activity. For a forced degradation study, expose promethazine API (10 mg) to UV light for 24 h. Analyze by HPLC. The impurity peak will appear. No cell culture is required.
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| Animal Protocol |
General protocol for in vivo animal experiments: Not applicable for efficacy. For a toxicokinetic study of promethazine, administer promethazine (10 mg/kg, IP) to rats. Collect plasma. Extract and analyze by LC-MS/MS. The method must be capable of separating and quantifying this impurity. The impurity is not dosed directly.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: This compound (MW 320.88) is the HCl salt of a small molecule (free base MW 284.42). It is not a drug. It is soluble in water and methanol. For storage, the reference standard is supplied as a solid and should be stored at -20degC. The product is for research and quality control use only. It is an impurity of Promethazine and is used as a reference standard. The product is for research use only and not for human consumption.
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| Toxicity/Toxicokinetics |
General toxicity profile: As an impurity, it is controlled to low levels (<0.1-0.5%). Standard chemical handling safety precautions (gloves, lab coat, safety glasses) should be used. This compound is a promethazine impurity and is for research and forensic applications only. It is a white to off-white solid. For research use only.
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| References |
| Molecular Formula |
C17H21CLN2S
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|---|---|
| Molecular Weight |
320.88
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| Exact Mass |
320.111
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| CAS # |
5568-90-1
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| PubChem CID |
110668
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
298
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CN(C)C)N1C2=CC=CC=C2SC3=CC=CC=C31.Cl
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| InChi Key |
RISCHQYUHLQSBU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N2S.ClH/c1-13(12-18(2)3)19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H
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| Chemical Name |
N,N-dimethyl-2-phenothiazin-10-ylpropan-1-amine;hydrochloride
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| Synonyms |
Isopromethazine hydrochloride standard
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 3.1164 mL | 15.5821 mL | 31.1643 mL | |
| 5 mM | 0.6233 mL | 3.1164 mL | 6.2329 mL | |
| 10 mM | 0.3116 mL | 1.5582 mL | 3.1164 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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