[CAS NO. 150322-43-3]  Prasugrel

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PRODUCTS SPECIFICATIONS [150322-43-3]

Catalog
HY-15284
Brand
MCE
CAS
150322-43-3

DESCRIPTION [150322-43-3]

Overview

MDLMFCD09954140
Molecular Weight373.44
Molecular FormulaC20H20FNO3S
SMILESFC1=CC=CC=C1C(C(C2CC2)=O)N3CCC4=C(C3)C=C(S4)OC(C)=O

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

Summary

Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation [1] .


IC50 & Target

P2Y12 receptor [1]


In Vivo

In rat platelets, Prasugrel active metabolite inhibits in vitro platelet aggregation induced by adenosine ADP (10μM) with an IC 50 value of 1.8 μM [2] .
Prasugrel acts faster and is significantly more potent than Clopidogrel in vivo. Prasugrel is an inactive prodrug that requires metabolic processing in vivo to generate the active antiplatelet metabolite. Prasugrel is rapidly absorbed from the gut. After oral administration of standard-loading doses of 60 mg, maximum plasma levels of the active metabolite are achieved within 1 h, effective, maximum inhibition of platelet aggregation at 1-2 h [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02285751 Medical University of Vienna
Critical Illness
November 2012 Phase 2
NCT00357968 Eli Lilly and Company|Daiichi Sankyo, Inc.|The TIMI Study Group
Coronary Artery Disease
August 2006 Phase 2
NCT01175200 Ascopharm Groupe Novasco|Groupe Hospitalier Pitie-Salpetriere|Medco Health Solutions, Inc.
Anti Platelet Effects
September 2010 Not Applicable

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 : 100 mg/mL ( 267.78 mM ; Need ultrasonic)

H 2 O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6778 mL 13.3890 mL 26.7781 mL
5 mM 0.5356 mL 2.6778 mL 5.3556 mL
10 mM 0.2678 mL 1.3389 mL 2.6778 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: ≥ 2.5 mg/mL (6.69 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

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


Synonyms

Ethanone, 2-[2-(acetyloxy)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)-
Thieno[3,2-c]pyridine, ethanone deriv.
2-[2-(Acetyloxy)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone
CS 747
Prasugrel
2-Acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
LY 640315
Effient free base
2-Acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine
[5-[2-Cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-2-yl] acetate