Home Metabolism Prostaglandin Receptor antagonist Ramatroban

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Ramatroban Prostaglandin Receptor antagonist

Cat.No.S5286

Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells.
Ramatroban Prostaglandin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 416.47

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Quality Control

Batch: Purity: 99.50%
99.50

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 416.47 Formula

C21H21FN2O4S

 Storage (From the date of receipt)
CAS No. 116649-85-5 -- Storage of Stock Solutions

Synonyms BAY u 3405 Smiles C1CC2=C(CC1NS(=O)(=O)C3=CC=C(C=C3)F)C4=CC=CC=C4N2CCC(=O)O

Mechanism of Action

Targets/IC50/Ki
TxA2 receptor
In vitro
Ramatroban can block the PGD2 receptor, chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). This compound can suppress the expression of monocyte chemoattractant protein-1 (MCP-1) and adhesion molecules in endothelial cells and prevent exacerbation of inflammation by blocking these responses. It has inhibitory effects on platelet aggregation and vascular smooth muscle contraction. This chemical significantly inhibited binding of [3H]PGD2 to CRTh2 with an IC50 value of 100 nM. It also inhibited, in a concentration-dependent manner, PGD2-induced Ca2+ mobilization in CRTh2 transfectants with an IC50 = 30 nM and suppressed migration of human eosinophils induced by PGD2 with an IC50 = 170 nM.
In vivo
In hypercholesterolemic rabbits, ramatroban prevents macrophage infiltration through MCP-1 downregulation and neointimal formation after balloon injury and attenuates vascular response to acetylcholine. The pharmacokinetic parameters after single oral administration of 75 mg of this compound were studied in fasting healthy adult volunteers: relative bioavailability of its tablets (as compared with aqueous solution) was 80.3%. The pharmacokinetics of this chemical at doses ranging from 25 to 150 mg was found to be linear. When a single dose of 50 mg of this agent was given orally to healthy volunteers postprandially, the AUC was 88.8% of that obtained in fasting state. A low total body clearance of this substance is shown in elderly subjects; After oral administration of [14C]-labeled material to male rats, maximum concentrations of radioactivity were higher in liver, kidneys and adipose tissues than in plasma. Other organs tissues had lower radioactivity levels than plasma. Radioactivity levels in most organs tissues declined in parallel with the decrease in the plasma radioactivity. In contrast, elimination of the radioactivity from the blood cells was relatively prolonged. Extremely low radioactivity levels were found only in the brain. The ratio of brain-to-plasma levels was as low as 8% at the maximum.
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