Roxatidine Acetate hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Roxatidine Acetate Hydrochloride 是一种特异性、竞争性组胺 H2 受体拮抗剂，IC50 为 3.2 μM。

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. (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.

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 264.7Concentration:40, 80, and 120 μM Incubation Time:1 hResult: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).

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.

HOE 760 | TZU-0460

GPCR/G Protein

Histamine Receptor

H2 receptor

Inflammation/Immunology

——

93793-83-0

384.9

C19H29ClN2O4

>98% (HPLC)

Ethanol: 12 mg/mL (31.17 mM); Water: 77 mg/mL (200.05 mM); DMSO: 77 mg/mL (200.05 mM)

CC(=O)OCC(=O)NCCCOC1=CC=CC(=C1)CN2CCCCC2.Cl

[2-oxo-2-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]ethyl] acetate;hydrochloride

(-20℃)

With Ice Pack

≥ 2 years