Elarofiban

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 328089

CAS#: 198958-88-2

Description: Elarofiban, also known as RWJ-53308, is a potent, selective and orally active GPIIb/IIIa antagonist. 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). RWJ-53308 may be useful for both acute and chronic treatment of arterial thrombotic disorders.

Chemical Structure

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Elarofiban
CAS# 198958-88-2
Instruction

Theoretical Analysis

MedKoo Cat#: 328089
Name: Elarofiban
CAS#: 198958-88-2
Chemical Formula: C22H32N4O4
Exact Mass: 416.24
Molecular Weight: 416.522
Elemental Analysis: C, 63.44; H, 7.74; N, 13.45; O, 15.36

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Elarofiban; RWJ-53308; RWJ 53308; RWJ53308.

IUPAC/Chemical Name: (S)-beta-((R)-1-(3-(4-Piperidyl)propionyl)nipecotamido)-3-pyridinepropionic acid

InChi Key: ABNXKGFLZFSILK-MOPGFXCFSA-N

InChi Code: InChI=1S/C22H32N4O4/c27-20(6-5-16-7-10-23-11-8-16)26-12-2-4-18(15-26)22(30)25-19(13-21(28)29)17-3-1-9-24-14-17/h1,3,9,14,16,18-19,23H,2,4-8,10-13,15H2,(H,25,30)(H,28,29)/t18-,19+/m1/s1

SMILES Code: O=C(O)C[C@H](NC([C@@H]1CCCN(C(CCC2CCNCC2)=O)C1)=O)C3=CC=CN=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 416.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Markowska M, Oberle R, Juzwin S, Hsu CP, Gryszkiewicz M, Streeter AJ.
Optimizing Caco-2 cell monolayers to increase throughput in drug intestinal
absorption analysis. J Pharmacol Toxicol Methods. 2001 Jul-Aug;46(1):51-5. PubMed
PMID: 12164260.


2: Damiano BP, Mitchell JA, Giardino E, Corcoran T, Haertlein BJ, de Garavilla L,
Kauffman JA, Hoekstra WJ, Maryanoff BE, Andrade-Gordon P. Antiplatelet and
antithrombotic activity of RWJ-53308, a novel orally active glycoprotein IIb/IIIa
antagonist. Thromb Res. 2001 Oct 15;104(2):113-26. PubMed PMID: 11672755.


3: Lawson EC, Hoekstra WJ, Addo MF, Andrade-Gordon P, Damiano BP, Kauffman JA,
Mitchell JA, Maryanoff BE. 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. PubMed PMID: 11551763.


4: Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo
MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF,
Mitchell JA, Scott L, Shah RD, Yabut SC. Potent, orally active GPIIb/IIIa
antagonists containing a nipecotic acid subunit. Structure-activity studies
leading to the discovery of RWJ-53308. J Med Chem. 1999 Dec 16;42(25):5254-65.
PubMed PMID: 10602710.