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BD0379945

Ramatroban , 98% , 116649-85-5

Synonym(s):
(+)-(3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid;BAY u3405

CAS NO.:116649-85-5

Empirical Formula: C21H21FN2O4S

Molecular Weight: 416.47

MDL number: MFCD00887606

Pack Size Price Stock Quantity
10mg RMB349.60 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 134-135°
alpha  D +70.1° (c = 1.0 in methanol)
Boiling point: 654.7±65.0 °C(Predicted)
Density  1.43±0.1 g/cm3(Predicted)
storage temp.  Sealed in dry,2-8°C
solubility  DMSO: ≥40mg/mL
form  solid
pka 4.60±0.10(Predicted)
color  white

Description and Uses

Ramatroban, originally developed for the treatment of cardiovascular pathologies as thromboembolism, was finally introduced in Japan for the treatment of allergic rhinitis. It is a (3R)-enantiomer that can be synthesized in 5 steps from 3-oxo-1,2,3,4- tetrahydrocarbazole by stereoselective reductive amination, using S-phenethylamine as the chiral source, followed by hydrogenolysis, sulfonylation and finally 2-step Ncarboxyethylation. Ramatroban is a potent antagonist of prostaglandin receptors (PGD2, PGH2) and thromboxane receptors (TxA2); accordingly, it blocks the contractions induced by thromboxane or TxA2-mimetics in animal and human airway smooth muscle. It also prevents, when administered i.v., p.o. or by aerosol, bronchoconstriction induced by PGD2 or antigen. In animal models of nasal allergy, ramatroban inhibits antigen-induced neutrophil infiltration into nasal mucosa and also inhibits nasal symptoms. In several species including humans, it is well-absorbed, extensively protein-bound (>95%) and eliminated mainly as a glucuro-conjugate; in man, its terminal half-life is 2 to 3 hours.

A thromboxane receptor antagonist for use in the treatment of coronary artery disease.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P305+P351+P338
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26-36/37/39-45
WGK Germany  1

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