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Elarofiban

Catalog No. T27250 CAS 198958-88-2

Synonyms: RWJ-53308, RWJ 53308, RWJ53308

Elarofiban(RWJ-53308) is a novel and orally active GPIIb/IIIa antagonist.

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Elarofiban, CAS 198958-88-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 397.00
5 mg	In stock	$ 970.00
10 mg	In stock	$ 1,290.00
25 mg	In stock	$ 1,950.00
50 mg	In stock	$ 2,620.00
100 mg	In stock	$ 3,530.00

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Purity: 99.94%

ee: 99.66%

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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]

Synonyms	RWJ-53308, RWJ 53308, RWJ53308
Molecular Weight	416.51
Formula	C22H32N4O4
CAS No.	198958-88-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Hugenberg V, et al. GMP-Compliant Radiosynthesis of [18F]GP1, a Novel PET Tracer for the Detection of Thrombi. Pharmaceuticals (Basel). 2021 Jul 28;14(8):739. 2. Kim C, et al. Glycoprotein IIb/IIIa receptor imaging with 18F-GP1 positron emission tomography for acute venous thromboembolism: an open-label, non-randomized, first-in-human phase 1 study. J Nucl Med. 2018 Jun 29;60(2):244–9. 3. Lawson EC, et al. 1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22. 4. Damiano BP, et al. Antiplatelet and antithrombotic activity of RWJ-53308, a novel orally active glycoprotein IIb/IIIa antagonist. Thromb Res. 2001 Oct 15;104(2):113-26.

Related compound libraries

This product is contained In the following compound libraries：

Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Elarofiban 198958-88-2 Cytoskeletal Signaling Integrin RWJ-53308 RWJ 53308 RWJ53308 inhibitor inhibit

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