| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
H1 Receptor
Promethazine-d4 hydrochloride does not have a distinct pharmacological target separate from unlabeled Promethazine. Promethazine acts as a histamine H1 receptor antagonist (Ki = 0.98 nM for the human receptor) and also exhibits anticholinergic and antiemetic properties. |
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
As a deuterated internal standard, Promethazine-d4 hydrochloride does not exhibit pharmacological activity distinct from that of unlabeled Promethazine. The deuterium labeling does not significantly alter the biological activity of the compound. Promethazine itself is a potent H1 receptor antagonist that blocks the effects of histamine, and also has anticholinergic and antiemetic effects. In research applications, the deuterated form is used for analytical purposes and is not typically used in functional assays to study its pharmacological activity. |
| ln Vivo |
Promethazine-d4 hydrochloride is not used as a pharmacologically active compound in vivo. Unlabeled Promethazine is used clinically as an antihistamine, antiemetic, and sedative. It is well-absorbed and widely distributed, crossing the blood-brain barrier to exert its central effects. Promethazine-d4 is used as an internal standard in pharmacokinetic studies to accurately measure the concentration of Promethazine in biological samples.
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| Enzyme Assay |
In vitro receptor binding assays are not typically performed with Promethazine-d4 hydrochloride as it is used as an analytical standard. However, for unlabeled Promethazine, radioligand binding studies using membrane preparations from cells expressing the H1 receptor are conducted to determine its binding affinity. The compound's ability to displace a specific radiolabeled H1 antagonist, such as [3H]-mepyramine, is measured to calculate its Ki value (0.98 nM for the human receptor).
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| Cell Assay |
In vitro cell-based assays are not typically performed with Promethazine-d4 hydrochloride as it is used as an analytical standard. Unlabeled Promethazine is used in cell-based assays to study its antihistamine and anticholinergic effects. These assays involve treating cells expressing H1 or muscarinic receptors with Promethazine and measuring its ability to inhibit agonist-induced responses.
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| Animal Protocol |
In vivo animal studies are not typically performed with Promethazine-d4 hydrochloride as it is used as an analytical standard. Unlabeled Promethazine is used in animal models to study its antihistamine, antiemetic, and sedative effects. Promethazine-d4 is used as an internal standard in pharmacokinetic studies in animals to quantify the concentration of Promethazine in blood, plasma, or tissues.
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| ADME/Pharmacokinetics |
Promethazine-d4 hydrochloride is used as an internal standard for the quantification of promethazine in biological matrices using GC-MS or LC-MS. As a deuterated compound, it exhibits practically identical chemical properties to unlabeled Promethazine, making it an ideal internal standard. Its use improves the accuracy and precision of analytical methods by correcting for variations in sample preparation, injection volume, and ionization efficiency. The compound is stable under recommended storage conditions (4°C, sealed from moisture).
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for Promethazine-d4 hydrochloride. As a deuterated form of Promethazine, its toxicity profile is expected to be similar to that of unlabeled Promethazine. Promethazine is generally well-tolerated, but common side effects include drowsiness, dizziness, dry mouth, and blurred vision. At higher doses, it may cause more severe anticholinergic effects and central nervous system depression. The deuterium labeling does not introduce any additional toxicity.
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| References |
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| Additional Infomation |
Promethazine-d4 hydrochloride is a deuterated analog of Promethazine, a first-generation antihistamine. It is intended for use as an internal standard for the quantification of promethazine by GC- or LC-MS. The compound features the replacement of four hydrogen atoms with deuterium, providing a distinct mass shift for accurate mass spectrometry analysis. It is not a therapeutic agent and is strictly for research purposes. The compound is sensitive to light and should be stored appropriately.
|
| Molecular Formula |
C17H17D4CLN2S
|
|---|---|
| Molecular Weight |
324.90
|
| Exact Mass |
324.137
|
| CAS # |
1173018-74-0
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| Related CAS # |
Promethazine hydrochloride;58-33-3
|
| PubChem CID |
71312314
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| Appearance |
Off-white to yellow solid powder
|
| LogP |
5.106
|
| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
|
| Complexity |
298
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C1=CC(=C2C(=C1)SC3=CC(=CC(=C3N2CC(C)N(C)C)[2H])[2H])[2H].Cl
|
| InChi Key |
XXPDBLUZJRXNNZ-RPMJCVFWSA-N
|
| InChi Code |
InChI=1S/C17H20N2S.ClH/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H/i6D,7D,8D,9D;
|
| Chemical Name |
N,N-dimethyl-1-(1,3,7,9-tetradeuteriophenothiazin-10-yl)propan-2-amine;hydrochloride
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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 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)
|
| 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 | 3.0779 mL | 15.3894 mL | 30.7787 mL | |
| 5 mM | 0.6156 mL | 3.0779 mL | 6.1557 mL | |
| 10 mM | 0.3078 mL | 1.5389 mL | 3.0779 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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