| Name | Elarofiban |
| Description | Elarofiban(RWJ-53308) is a novel and orally active GPIIb/IIIa antagonist. |
| In vitro | Elarofiban (RWJ-53308) is a novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist that inhibits fibrinogen binding to GPIIb/IIIa with an IC(50) of 0.4+/-0.3 nM. RWJ-53308 inhibits thrombin-induced platelet aggregation in human gel-filtered platelets (IC(50)=60+/-12 nM) and platelet aggregation in human platelet-rich plasma (PRP) in response to collagen, arachidonic acid, ADP, and SFLLRN-NH(2) (IC(50)=60+/-10, 150+/-30, 70+/-4, and 160+/-80 nM, respectively).[4] |
| In vivo | The potency of Elarofiban (RWJ-53308) in dog and guinea pig PRP is similar to human PRP. RWJ-53308 inhibits ex vivo collagen- and ADP-induced platelet aggregation in conscious dogs for up to 4 h following 0.3 mg/kg iv, and through 4 and 6 h following 1 and 3 mg/kg po. Oral bioavailability is 16+/-7%. RWJ-53308 reduces thrombus weight in a canine arteriovenous (AV) shunt model following intravenous (0.01-0.1 mg/kg) and oral (3 mg/kg) administration. In a guinea pig carotid artery pinch-injury model, RWJ-53308 completely suppresses thrombus-induced cyclic flow reductions (CFR) at 0.7 mg/kg iv. RWJ-53308 also blocks thrombus formation in photoactivation- and ferric chloride-induced models of thrombosis in guinea pigs at 0.3 and 1 mg/kg iv, respectively. In summary, RWJ-53308 is a potent orally active GPIIb/IIIa antagonist that may be useful for both acute and chronic treatment of arterial thrombotic disorders.[4] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (144.05 mM), Sonication is recommended.
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| Keywords | GPIIb/IIIa | Elarofiban |
| Inhibitors Related | K34c hydrochloride | Cucurbitacin B | Tirofiban hydrochloride monohydrate | (R)-Leucic acid | Lifitegrast | Cyclo(-RGDfK) | ADH-503 | Elsibucol | CLT-28643 | Bestatin hydrochloride | Gantofiban | 2-hydroxy Flutamide |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Human Metabolite Library |
United States
