PF-06427878
PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases.
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- CAS No.: 1809064-23-0
- Formule: C26H28N4O5
- Masse moléculaire:476.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1809064-23-0
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Masse moléculaire 476.52
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Formule C26H28N4O5
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SMILES
O=C(O)C1=CC=CC(CNC(C2=CN=C(N3C[C@H](OC4=CC=CC=C4OCC)CCC3)N=C2)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Amin NB, et al. Targeting diacylglycerol acyltransferase 2 for the treatment of nonalcoholic steatohepatitis. Sci Transl Med. 2019 Nov 27;11(520):eaav9701. [Content Brief]
[2]. Sharma R, et al. Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate Ervogastat. Chem Res Toxicol. 2023 Jun 19;36(6):934-946. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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