[CAS NO. 936500-94-6] Elinogrel

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PRODUCTS SPECIFICATIONS [936500-94-6]

Catalog

HY-11021

Brand

MCE

CAS

936500-94-6

DESCRIPTION [936500-94-6]

Overview

MDL	-
Molecular Weight	523.95
Molecular Formula	C20H15ClFN5O5S2
SMILES	O=S(C1=CC=C(Cl)S1)(NC(NC2=CC=C(N3C(NC4=C(C=C(F)C(NC)=C4)C3=O)=O)C=C2)=O)=O

For research use only. We do not sell to patients.

Summary

Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y ₁₂ antagonist ( IC ₅₀ =20 nM). It is orally and intravenously available and has potent antiplatelet effects ^[1] .

IC50 & Target

IC50: 20 nM (P2Y ₁₂ ) ^[2]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00751231	Portola Pharmaceuticals	Percutaneous Coronary Intervention	December 2008	Phase 2
NCT00984113	Portola Pharmaceuticals\|Novartis	Renal Impairment	September 2009	Phase 1
NCT00546260	Portola Pharmaceuticals	Myocardial Infarction	November 2007	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL ( 119.29 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9086 mL	9.5429 mL	19.0858 mL
5 mM	0.3817 mL	1.9086 mL	3.8172 mL
10 mM	0.1909 mL	0.9543 mL	1.9086 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

2-Thiophenesulfonamide, 5-chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]-

5-Chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]-2-thiophenesulfonamide

PRT 060128

Elinogrel

N-[4-(6-Fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)phenyl]-N′-[(5-chlorothiophen-2-yl)sulfonyl]urea

1-(5-Chlorothiophen-2-yl)sulfonyl-3-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1H-quinazolin-3-yl]phenyl]urea