Cat. No.: HY-B0305A

Roxatidine Acetate Hydrochloride

(Synonyms: HOE 760)

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Based on 1 Customer Validation

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.

Purity: 99.57%
CAS No.: 93793-83-0
Formula: C₁₉H₂₉ClN₂O₄
Molecular Weight:384.90

Storage:

4°C, sealed storage, away from moisture

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

Roxatidine Acetate Hydrochloride Chemical Structure

CAS No.: 93793-83-0

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

H₂ Receptor

All Histamine Receptor Isoforms :

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.

Chemical Information

CAS No. 93793-83-0
Appearance Solid
Molecular Weight 384.90
Formula C₁₉H₂₉ClN₂O₄
Color White to off-white
SMILES

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

HOE 760
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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5981 mL

12.9904 mL

25.9808 mL

5 mM

0.5196 mL

2.5981 mL

5.1962 mL

10 mM

0.2598 mL

1.2990 mL

2.5981 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

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In Vivo:

Working Solution

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Murdoch D, et al. Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders. Drugs. 1991 Aug;42(2):240-60. [Content Brief]

[2]. Cho EJ, et al. Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages. J Cell Biochem. 2011 Dec;112(12):3648-59. [Content Brief]

[3]. Tomita K, et al. Roxatidine- and cimetidine-induced angiogenesis inhibition suppresses growth of colon cancer implants in syngeneic mice. J Pharmacol Sci. 2003 Nov;93(3):321-30. [Content Brief]

[4]. Minho Lee, et al. Roxatidine attenuates mast cell-mediated allergic inflammation via inhibition of NF-κB and p38 MAPK activation. Sci Rep. 2017 Jan 31;7:41721. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Roxatidine Acetate Hydrochloride Related Classifications

HY-B0305A Related Classifications