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Roxatidine

CAS No.78273-80-0
Chemical Name:Roxatidine
CBNumber:CB1472068
Molecular Formula:C17H26N2O3
Formula Weight:306.4
MOL File:78273-80-0.mol

Roxatidine Property

Melting point 59-60 °C
Boiling point 524.3±45.0 °C(Predicted)
Density 1.137±0.06 g/cm3(Predicted)
storage temp. -20°
solubility Soluble in DMSO (up to 25 mg/ml).
pka 13.34±0.10(Predicted)
form oil
color Colorless to pale yellow
Stability Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
CAS DataBase Reference 78273-80-0(CAS DataBase Reference)
FDA UNII IV9VHT3YUM
ATC code A02BA06

Safety

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H302
Precautionary statements P264-P270-P301+P312-P330-P501

Roxatidine Chemical Properties,Usage,Production

Description Roxatidine (78273-80-0) is a novel histamine H2 receptor antagonist.1?Suppresses inflammatory responses via inhibition of NFκB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages.2?Clinically useful agent for prevention and healing of gastric and duodenal ulcers and bleeding.3?Attenuates degradation of extracellular matrix in osteoarthritis models by inactivating the NFkB pathway.4
Uses Anti-ulcerative.

in vivo

Roxatidine (20 mg/kg, p.o., a single dose for 1h before Compound 48/80 injection) ameliorates Compound 48/80 (HY-115768) (8mg/kg, i.p., a single dose for 1h)-induced allergic hypersensitivity and suppresses Compound 48/80-induced allergic inflammation in anaphylactic animal model^[1].

Animal Model:	Compound 48/80-induced anaphylactic shock mouse model^[1]
Dosage:	20 mg/kg
Administration:	p.o., a single dose for 1h before Compound 48/80 injection
Result:	Increased the survival rate to 20% at 60 min after compound 48/80 injection.

IC 50 H₂ Receptor
References 1) Mills and Wood (1989),?The pharmacology of histamine H2-receptor antagonists; Methods Find. Exp. Clin. Pharmacol., 11 Suppl. 1?87 2) Cho?et al. (2011), Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages; J. Cell. Biochem.,?112?3648 3) Imaeda?et al.?(2011),?Effect of lansoprazole versus roxatidine on prevention of bleeding and promotion of ulcer healing after endoscopic submucosal dissection for superficial gastric neoplasia; J. Gastroenterol.,?46?1267 4) Ze?et al. (2017),?Roxatidine Attenuates Degradation of Extracellular Matrix;?Biomed. Pharmacother.,?95?1156