2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Ranitidine

Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice.

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Ranitidine Chemical Structure

Ranitidine Chemical Structure

CAS No. : 66357-35-5

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Based on 1 publication(s) in Google Scholar

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Ranitidine Related Antibodies

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Description

Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice[1][2].

IC50 & Target[1][2]

H2 Receptor

 

In Vivo

Ranitidine (0.03-3 mg/kg; i.v.; once) inhibits Histamine (HY-B1204)- and Pentagastrin (HY-A0261)-induced gastric acid secretion in the perfused stomach preparation of the anaesthetized rat[1].
Ranitidine (8 mg/kg; oral administration; administered every other day; treatment for 8 days) reduces the number of CD11b+Ly6Chi cells in the spleen and bone marrow of BALB/c mice[2].
Ranitidine (8 mg/kg; oral administration; administered every other day; treatment for 8 days) inhibits lung metastasis in BALB/c mice bearing 4T1 breast cancer[2].
Ranitidine (8 mg/kg; oral administration; administered every other day; for 14 days) inhibits primary tumor growth in the E0771 breast cancer model of C57BL/6 mice[2].
Ranitidine (dose enabling mice to ingest 6-8 mg/kg per day; added to drinking water; changed every 3 days; treatment starting from weaning (~4 weeks) until the end of the experiment (23-26 weeks)) increases the latency of breast tumorigenesis and reduces the number of tumors in LKB1-/-NIC mice[2].

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

Animal Model: Female Wistar rats (100 to 120 g) were anaesthetized with sodium pentobarbitone (50 mg/kg i.p.), and intravenous with Histamine (100 μg/kg/min) or Pentagastrin (1 μg/kg/min)[1].
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 0.6 mg/kg, 1 mg/kg, 3 mg/kg
Administration: i.v.; once
Result: Inhibited Histamine- and Pentagastrin-induced gastric acid secretion in the perfused stomach preparation of the anaesthetized rat.
Animal Model: BALB/c female mice (5-6-8 week old), orthotopic breast cancer model by injecting 100,000 4T1 cells subcutaneously into the mammary fat pad near the fourth nipple[2].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased the proportion of CD11b+Ly6Chi monocytic cells in the spleen and inhibited lung metastasis.
Animal Model: C57BL/6 female mice (6-8 week old), orthotopic breast cancer model by injecting 200,000 E0771 cells in 100 μL of Matrigel subcutaneously into the mammary fat pad near the fourth nipple[2].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased primary tumor growth starting from approximately day 13 post-tumor cell injection.
Animal Model: LKB1-/-/NIC female mice (weaned at about 4 weeks old), spontaneous tumor development model starting from weaning[2].
Dosage: 6-8 mg/kg
Administration: Oral administration, every 3 days, from weaning until the end of the experiment
Result: Increased the latency of tumorigenesis by an additional 24 days and reduced the average number of tumors per mouse.
Clinical Trial
Molecular Weight

314.40

Formula

C13H22N4O3S
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

O=[N+](/C=C(NC)/NCCSCC1=CC=C(CN(C)C)O1)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (318.07 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 3.1807 mL 15.9033 mL 31.8066 mL
5 mM 0.6361 mL 3.1807 mL 6.3613 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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 (7.95 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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.
Purity & Documentation

Purity: ≥99.0%

SDS (393 KB)

COA (244 KB)

Handling Instructions (2659 KB)
References

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 (protect from light, stored under nitrogen). 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 3.1807 mL 15.9033 mL 31.8066 mL 79.5165 mL
5 mM 0.6361 mL 3.1807 mL 6.3613 mL 15.9033 mL
10 mM 0.3181 mL 1.5903 mL 3.1807 mL 7.9517 mL
15 mM 0.2120 mL 1.0602 mL 2.1204 mL 5.3011 mL
20 mM 0.1590 mL 0.7952 mL 1.5903 mL 3.9758 mL
25 mM 0.1272 mL 0.6361 mL 1.2723 mL 3.1807 mL
30 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6506 mL
40 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9879 mL
50 mM 0.0636 mL 0.3181 mL 0.6361 mL 1.5903 mL
60 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9940 mL
100 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL
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Ranitidine Related Classifications

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:

Ranitidine66357-35-5Histamine ReceptorGastricsecretionH2-receptororallyCYP2C19CYP2C9Inhibitorinhibitorinhibit

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