Promethazine
Based on 1 publication(s) in Google Scholar
Promethazine is an orally active histamine receptor antagonist. Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 60-87-7
- Formula: C17H20N2S
- Molecular Weight:284.42
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Promethazine
MoreAll Histamine Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
35.1 μM
Compound: promethazine
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
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[PMID: 18788725] |
| HT-1080 | EC50 |
0.264 μM
Compound: promethazine
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Inhibition of erastin-induced ferroptosis in human HT-1080 cells assessed as cell viability incubated for 48 hrs by MTT assay
Inhibition of erastin-induced ferroptosis in human HT-1080 cells assessed as cell viability incubated for 48 hrs by MTT assay
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[PMID: 33065375] |
| HT-29 | IC50 |
27.34 μM
Compound: 40; PMTZ
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK-8 method
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK-8 method
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[PMID: 38142509] |
| NCI-H1650 | GI50 |
>40 μM
Compound: Promethazine
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Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 26372073] |
| ScN2a | EC50 |
8 μM
Compound: Promethazine
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Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
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[PMID: 12904059] |
| SW480 | IC50 |
33 μM
Compound: 40; PMTZ
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Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK-8 method
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 24 hrs by CCK-8 method
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[PMID: 38142509] |
Promethazine (0-100 μM, 24 h) inhibits the proliferation of SW480, HCT116, HT29 and Caco2 CRC cells in a concentration-dependent manner[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480, HCT116, HT29, and Caco2 CRC cells
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Concentration:0-100 μM
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Incubation Time:24 hours
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Result:Exhibited IC50 values of 40.96, 74.79, 27.34 and 33.00 μM in Caco2, HCT116, HT29 and SW480 cells, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI mice (20-30 g) injected with acetic acid (0.7%)[6]
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Dosage:2 mg/kg, 4 mg/kg, 6 mg/kg
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Administration:Intraperitoneal injection; 2 mg/kg, 4 mg/kg, 6 mg/kg; once
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Result:Inhibited writhing response by 43.2%, 53.9% and 62.3% at 2, 4, 6 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 60-87-7
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Appearance Solid
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Molecular Weight 284.42
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Formula C17H20N2S
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Color White to off-white
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SMILES
CC(N(C)C)CN1C2=C(C=CC=C2)SC3=CC=CC=C31
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Synonyms
(±)-Promethazine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351
Solvent & Solubility
DMSO : 100 mg/mL (351.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Burt DR, et al. Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science. 1977 Apr 15;196(4287):326-8. [Content Brief]
[2]. Strenkoski-Nix LC, et al. Pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories and oral syrup to healthy subjects. Am J Health Syst Pharm. 2000 Aug 15;57(16):1499-505. [Content Brief]
[3]. Fiorella D, et al. The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis. Psychopharmacology (Berl). 1995 Oct;121(3):347-56. [Content Brief]
[4]. Seeman P, et al. Dopamine D2 receptor binding sites for agonists. A tetrahedral model. Mol Pharmacol. 1985 Nov;28(5):391-9. [Content Brief]
[5]. Xinyue Tan, et al. Promethazine inhibits proliferation and promotes apoptosis in colorectal cancer cells by suppressing the PI3K/AKT pathway. Biomed Pharmacother. 2021 Nov;143:112174. [Content Brief]
[6]. Niloofar Amidi, et al. A Behavioral Study of Promethazine Interaction with Analgesic Effect of Diclofenac: Pain Combination Therapy. J Pharmacopuncture. 2020 Mar 31;23(1):18-24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5159 mL | 17.5796 mL | 35.1593 mL | 87.8982 mL |
| 5 mM | 0.7032 mL | 3.5159 mL | 7.0319 mL | 17.5796 mL | |
| 10 mM | 0.3516 mL | 1.7580 mL | 3.5159 mL | 8.7898 mL | |
| 15 mM | 0.2344 mL | 1.1720 mL | 2.3440 mL | 5.8599 mL | |
| 20 mM | 0.1758 mL | 0.8790 mL | 1.7580 mL | 4.3949 mL | |
| 25 mM | 0.1406 mL | 0.7032 mL | 1.4064 mL | 3.5159 mL | |
| 30 mM | 0.1172 mL | 0.5860 mL | 1.1720 mL | 2.9299 mL | |
| 40 mM | 0.0879 mL | 0.4395 mL | 0.8790 mL | 2.1975 mL | |
| 50 mM | 0.0703 mL | 0.3516 mL | 0.7032 mL | 1.7580 mL | |
| 60 mM | 0.0586 mL | 0.2930 mL | 0.5860 mL | 1.4650 mL | |
| 80 mM | 0.0439 mL | 0.2197 mL | 0.4395 mL | 1.0987 mL | |
| 100 mM | 0.0352 mL | 0.1758 mL | 0.3516 mL | 0.8790 mL |
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