Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H11Cl2N3O |
Molecular Weight | 284.141 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)N2CC3=C(NC2=NC1=O)C=CC(Cl)=C3Cl
InChI
InChIKey=IGMDPBNGNRHCRW-UHFFFAOYSA-N
InChI=1S/C12H11Cl2N3O/c1-12(2)10(18)16-11-15-8-4-3-7(13)9(14)6(8)5-17(11)12/h3-4H,5H2,1-2H3,(H,15,16,18)
Molecular Formula | C12H11Cl2N3O |
Molecular Weight | 284.141 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24553755
4 mg/day for 14 days
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:01:24 GMT 2023
by
admin
on
Sat Dec 16 18:01:24 GMT 2023
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Record UNII |
V8Q1Z0GK92
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C1327
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V8Q1Z0GK92
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135564921
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C152145
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1029711-88-3
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DTXSID30145594
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300000036844
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9494
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admin on Sat Dec 16 18:01:24 GMT 2023 , Edited by admin on Sat Dec 16 18:01:24 GMT 2023
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ACTIVE MOIETY |