Roxatidine Acetate Hydrochloride (Synonyms: HOE 760)

Cat. No.: HY-B0305A Purity: 98.08%: FAQs
Data Sheet SDS 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

CAS No. : 93793-83-0

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Solution
10 mM * 1 mL in DMSO	USD 85	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 85	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
1 g	USD 130	In-stock	Estimated Time of Arrival: December 31
5 g	USD 370	In-stock	Estimated Time of Arrival: December 31
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50 g		Get quote

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Other Forms of Roxatidine Acetate Hydrochloride:

Roxatidine acetate Get quote

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Biological Activity
Purity & Documentation
References
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Description

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].

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].

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

Appearance

Solid

Formula

C₁₉H₂₉ClN₂O₄

CAS No.

93793-83-0

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)

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
10 mM	0.2598 mL	1.2990 mL	2.5981 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS
Solubility: 140 mg/mL (363.73 mM); Clear solution; Need ultrasonic

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (243 KB) LCMS (107 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]

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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Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

Roxatidine Acetate93793-83-0HOE 760HOE760HOE-760Histamine Receptorgastricduodenal ulceresteraseInhibitorinhibitorinhibit

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