盐酸罗沙替丁醋酸酯

概述生物活性靶点体外研究体内研究盐酸罗沙替丁醋酸酯试剂级价格

盐酸罗沙替丁醋酸酯

CAS号:93793-83-0
英文名:Roxatidine acetate hydrochloride
中文名:盐酸罗沙替丁醋酸酯
CBNumber:CB2179214
分子式:C19H29ClN2O4
分子量:384.89756
MOL File:93793-83-0.mol

盐酸罗沙替丁醋酸酯化学性质

熔点 :145-146°
储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
溶解度 :DMSO: 78 mg/ml; Ethanol: 12 mg/ml; Water: 77 mg/ml
形态 :powder to crystal
颜色 :White to Almost white
Merck :14,8274

安全信息

RTECS号 :AC3855000
海关编码 :2933.39.9200

盐酸罗沙替丁醋酸酯性质、用途与生产工艺

概述盐酸罗沙替丁醋酸酯在机体内通过醋解作用脱乙酰基转化为代谢物罗沙替丁。盐酸罗沙替丁醋酸酯和罗沙替丁都具有药效活性，可以有效抑制动物的基础胃酸分泌和刺激引起的胃酸分泌。
生物活性 Roxatidine Acetate HCl是特异性的，竞争性的组胺H2受体拮抗剂，IC50为3.2 μM，抑制胃酸分泌和溃疡形成。
靶点
Target Value
Histamine H2 receptor 3.2 μM
体外研究

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.

体内研究

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 decreases the compound 48/80-induced degradation of procaspase-1 and appearance of the corresponding cleaved bands in mice.

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.