Roxatidine Acetate hydrochloride

SKU: orb1223585

Description

Roxatidine Acetate hydrochloride is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation.(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.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.\n(In Vivo):Roxatidine Acetate Hydrochloride (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice.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.

Images & Validation

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Key Properties

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CAS Number	93793-83-0
MW	384.9
Purity	>98% (HPLC)
Formula	C₁₉H₂₉ClN₂O₄
SMILES	CC(=O)OCC(=O)NCCCOC1=CC=CC(=C1)CN2CCCCC2.Cl
Target	Histamine Receptor
Solubility	Ethanol: 12 mg/mL (31.17 mM); Water: 77 mg/mL (200.05 mM); DMSO: 77 mg/mL (200.05 mM)

Bioactivity

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In Vivo

Roxatidine Acetate Hydrochloride (0-300 mg/kg; p.o. ; 26 days) suppressed growth of Colon 38 tumor implants in mice. 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. Animal model: Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g). 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). Dosage: 20 mg/kg. Administration: Oral gavage; 20 mg/kg; single dose. Result: Suppressed compound 48/80-induced allergic inflammation in anaphylactic Animal model.

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. 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. Western blot analysis. 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).

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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HOE 760 | TZU-0460

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Gene Symbol

Histamine Receptor

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