ChemicalBook--->CAS DataBase List--->78273-80-0

78273-80-0

78273-80-0 Structure

78273-80-0 Structure
IdentificationMore
[Name]

Roxatidine
[CAS]

78273-80-0
[Synonyms]

n-{3-[3-(1-piperidinylmethyl)phenoxy]propyl}hydroxyacetamide
ROXATIDINE
ROXATIDINE ENTERPRISE STANDARD
RoxatidineAcetateHclBase
ROXATIDINE(SUBJECTTOPATENTFREE)
desacetyl-TZU-0460
2-Hydroxy-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]acetamide
2-Hydroxy-N-[3-[m-(piperidinomethyl)phenoxy]propyl]acetamide
[Molecular Formula]

C17H26N2O3
[MDL Number]

MFCD00871807
[Molecular Weight]

306.4
[MOL File]

78273-80-0.mol
Chemical PropertiesBack Directory
[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).
[form ]

oil
[pka]

13.34±0.10(Predicted)
[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)
Hazard InformationBack Directory
[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
[storage]

-20°C
[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
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