1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Roxatidine Acetate Hydrochloride

Roxatidine Acetate Hydrochloride  (Synonyms: HOE 760)

Cat. No.: HY-B0305A Purity: 99.26%
COA Handling Instructions

Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity.

For research use only. We do not sell to patients.

Roxatidine Acetate Hydrochloride Chemical Structure

Roxatidine Acetate Hydrochloride Chemical Structure

CAS No. : 93793-83-0

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
500 mg USD 77 In-stock
1 g USD 130 In-stock
5 g USD 370 In-stock
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  • Biological Activity

  • Purity & Documentation

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Description

Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity[1][2][3].

IC50 & Target[1]

H2 Receptor

 

In Vitro

Roxatidine Acetate Hydrochloride (0-120 μM, 1 h) suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages[2].
Roxatidine Acetate Hydrochloride (6.25  μM, 12.5 μM, and 25 μM; pre-treatment for 30 min) suppresses the PMACI-induced activation of p38 MAPK, but does not affect the phosphorylation of ERK or JNK. The total ERK 1/2, JNK, and p38 MAPK levels are unaffected by roxatidine in human mast-cells-1 (HMC-1) cells[4].

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

Western Blot Analysis[2]

Cell Line: RAW 264.7
Concentration: 40, 80, and 120 μM
Incubation Time: 1 h
Result: Suppressed LPS-induced PGE2, NO, and histamine production and COX-2, iNOS, and HDC expressions. Inhibited expressions of TNF-α, IL-1β, IL-6, and VEGF-1. Concentration-dependently attenuated the nuclear translocations of p65 and p50. Inhibited LPS-induced phosphorylation of p38 MAP kinase. Significantly down-regulated the LPS-induced productions of NO and PGE2 (prostaglandin E2).
In Vivo

Roxatidine Acetate Hydrochloride (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice[3].
Roxatidine Acetate Hydrochloride (oral gavage; 20 mg/kg; single dose) inhibits Compound 48/80-increased TNF-α, IL-6, and IL-1β production and mRNA expression. Additionally, Roxatidine Acetate Hydrochloride decreases the compound 48/80-induced degradation of procaspase-1 and appearance of the corresponding cleaved bands in mice[4].

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

Animal Model: Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g)[3]
Dosage: 30, 100, and 300 mg/kg per day, 1 ml/100 g body weight
Administration: Oral administration, 29 days beginning 3 days before Colon 38 implantation or 26 days beginning concomitantly with Colon 38 implantation
Result: Suppressed growth of Colon 38 tumor implants in a dose-related manner after day 26. Suppressed VEGF levels in tumor tissue and significantly decreased serum VEGF levels.
Animal Model: ICR male mice (6 weeks old)[1]
Dosage: 20 mg/kg
Administration: Oral gavage; 20 mg/kg; single dose
Result: Suppressed compound 48/80-induced allergic inflammation in anaphylactic animal model.
Molecular Weight

384.90

Formula

C19H29ClN2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)COC(C)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (129.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (129.90 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5981 mL 12.9904 mL 25.9808 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 140 mg/mL (363.73 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 (sealed storage, away from moisture). 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 / H2O 1 mM 2.5981 mL 12.9904 mL 25.9808 mL 64.9519 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL 12.9904 mL
10 mM 0.2598 mL 1.2990 mL 2.5981 mL 6.4952 mL
15 mM 0.1732 mL 0.8660 mL 1.7321 mL 4.3301 mL
20 mM 0.1299 mL 0.6495 mL 1.2990 mL 3.2476 mL
25 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5981 mL
30 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1651 mL
40 mM 0.0650 mL 0.3248 mL 0.6495 mL 1.6238 mL
50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8119 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Roxatidine Acetate Hydrochloride 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.

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Roxatidine Acetate Hydrochloride
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