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Technical Data
| Formula | C21H21FN2O4S |
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| Molecular Weight | 416.47 | CAS No. | 116649-85-5 | |
| Solubility (25°C)* | In vitro | DMSO | 42 mg/mL (100.84 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | 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. | |
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| Targets |
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| In vitro | Ramatroban can block the PGD2 receptor, chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). Ramatroban 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. Ramatroban 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[1]. | |
| 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 ramatroban were studied in fasting healthy adult volunteers: relative bioavailability of ramatroban tablets (as compared with aqueous solution) was 80.3%. The pharmacokinetics of ramatroban at doses ranging from 25 to 150 mg was found to be linear. When a single dose of 50 mg of ramatroban was given orally to healthy volunteers postprandially, the AUC was 88.8% of that obtained in fasting state. A low total body clearance of ramatroban is shown in elderly subjects; After oral administration of [14C]ramatroban 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[1]. |
Protocol (from reference)
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.