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 |
|
others | Enquire |
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 |