ACT-281959
ACT-281959 is an orally active prodrug of Selatogrel (HY-109122), a P2Y12 receptor antagonist. ACT-281959 can inhibit platelet aggregation and can be used for the research of cardiovascular disease.
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- CAS No.: 1159501-31-1
- 화학식: C38H55N6O14P
- 분자량:850.85
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
All P2Y Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
P2Y12 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
8 nM
Compound: ACT-281959
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Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 2 mins followed by ADP addition for 5 mins
Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 2 mins followed by ADP addition for 5 mins
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[PMID: 34731765] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1159501-31-1
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분자량 850.85
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화학식 C38H55N6O14P
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SMILES
O=C(N1CCN(C([C@@H](NC(C2=NC(C3=CC=CC=C3)=NC(N4C[C@@H](OC)CC4)=C2)=O)CP(OCOC(OC(C)C)=O)(OCOC(OC(C)C)=O)=O)=O)CC1)OCCCC
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
순도&문서
References
[1]. Caroff E, et al. 4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel. J Med Chem. 2015 Dec 10;58(23):9133-53. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ACT-281959 Related Classifications
HY-119085 Related Classifications
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