FK-788
FK-788 is a PGI(2) and IP agonist with a strong anti-aggregation effect, with an IC50 of 18 nM and a high binding affinity for the human recombinant IP receptor, with a Ki value of 20 nM.
For research use only. We do not sell to patients.
- CAS No.: 227951-89-5
- Formula: C26H25NO6
- Molecular Weight:447.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Cell line | IC50 |
18 nM
Compound: (R)-4: FK-788
|
Inhibition concentration against ADP-induced platelet aggregation using human platelet rich plasma
Inhibition concentration against ADP-induced platelet aggregation using human platelet rich plasma
|
[PMID: 15914004] |
| HEK293 | CC50 |
>20 μM
Compound: MMV1782352
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Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590)
Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590)
|
10.6019/CHEMBL4296181 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 227951-89-5
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Molecular Weight 447.48
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Formula C26H25NO6
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SMILES
O=C(O)COC1=C2CC[C@](O)(COC(N(C3=CC=CC=C3)C4=CC=CC=C4)=O)CC2=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Kouji Hattori, et al. Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3091-5. [Content Brief]
[2]. Fujiko Takamura, et al. Metabolism investigation leading to novel drug design 2: orally active prostacyclin mimetics. Part 5. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4475-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)