Promethazine (Synonyms: (±)-Promethazine)

Name: Promethazine
Brand: MedChemExpress
SKU: HY-B1296
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1296 Pureza: 99.67%: Ficha de datos
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Promethazine is an orally active histamine receptor antagonist. Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects.

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Promethazine Estructura química

No. CAS : 60-87-7

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Based on 1 publication(s) in Google Scholar

Other Forms of Promethazine:

Promethazine hydrochloride In-stock
(R)-Promethazine Obtener un presupuesto
Promethazine-d₆ hydrochloride Obtener un presupuesto
Promethazine-d₄ Obtener un presupuesto
Promethazine (Standard) Obtener un presupuesto

1 Publications Citing Use of MCE Promethazine

•PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Histamine Receptor:

Ver todas las isoformas

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

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Descripciòn

Promethazine is an orally active histamine receptor antagonist^[1]. Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects^[1]^[2]^[3]^[4].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	35.1 μM Compound: promethazine	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	[PMID: 18788725]
HT-1080	EC₅₀	0.264 μM Compound: promethazine	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	[PMID: 33065375]
HT-29	IC₅₀	27.34 μM Compound: 40; PMTZ	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	[PMID: 38142509]
NCI-H1650	GI₅₀	>40 μM Compound: Promethazine	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	[PMID: 26372073]
ScN2a	EC₅₀	8 μM Compound: Promethazine	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	[PMID: 12904059]
SW480	IC₅₀	33 μM Compound: 40; PMTZ	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	[PMID: 38142509]

In Vitro

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.

Cell Viability Assay^[5]

Cell Line:	SW480, HCT116, HT29, and Caco2 CRC cells
Concentration:	0-100 μM
Incubation Time:	24 hours
Result:	Exhibited IC₅₀ values of 40.96, 74.79, 27.34 and 33.00 μM in Caco2, HCT116, HT29 and SW480 cells, respectively.

In Vivo

Promethazine (intraperitoneal injection; 2 mg/kg, 4 mg/kg, 6 mg/kg; once) is effective in reducing the writhing response^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male NMRI mice (20-30 g) injected with acetic acid (0.7%)^[6]
Dosage:	2 mg/kg, 4 mg/kg, 6 mg/kg
Administration:	Intraperitoneal injection; 2 mg/kg, 4 mg/kg, 6 mg/kg; once
Result:	Inhibited writhing response by 43.2%, 53.9% and 62.3% at 2, 4, 6 mg/kg.

Ensayo clínico

Peso molecular

284.42

Fòrmula

C₁₇H₂₀N₂S

No. CAS

60-87-7

Appearance

Solid

Color

White to off-white

SMILES

CC(N(C)C)CN1C2=C(C=CC=C2)SC3=CC=CC=C31

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5159 mL	17.5796 mL	35.1593 mL
5 mM	0.7032 mL	3.5159 mL	7.0319 mL
10 mM	0.3516 mL	1.7580 mL	3.5159 mL

View the 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.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Pureza y Documentación

Purity: 99.67%

Select Batch:

Ficha de datos (280 KB) SDS (393 KB)

COA (255 KB) HNMR (263 KB) LCMS (103 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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

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

Promethazine Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Promethazine60-87-7(±)-PromethazineHistamine ReceptorHistamine Receptor AntagonistantihistamineSW480HCT116HT29Caco2Inhibitorinhibitorinhibit

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Promethazine (Synonyms: (±)-Promethazine)

Revisión del cliente

Other Forms of Promethazine:

Promethazine Related Antibodies

1 Publications Citing Use of MCE Promethazine

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Histamine Receptor:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Promethazine Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Promethazine Related Classifications

Keywords:

Productos vistos recientemente:

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SAFETY DATA SHEET (SDS)

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