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PF-06446846
CAS No. 1632250-49-7
PF-06446846( —— )
Catalog No. M22373 CAS No. 1632250-49-7
PF?06446846 is a potent and selective PCSK9 inhibitor?PF-06446846 reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.?
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 120 | In Stock |
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| 5MG | 176 | In Stock |
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| 10MG | 266 | In Stock |
|
| 25MG | 489 | In Stock |
|
| 50MG | 705 | In Stock |
|
| 100MG | 981 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NamePF-06446846
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NoteResearch use only, not for human use.
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Brief DescriptionPF?06446846 is a potent and selective PCSK9 inhibitor?PF-06446846 reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.?
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DescriptionPF?06446846 is a potent and selective PCSK9 inhibitor?PF-06446846 reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.?PF-06446846 is highly selective for the inhibition of PCSK9 translation.?The mechanism of action employed by PF-06446846 reveals a previously unexpected tunability of the human ribosome that allows small molecules to specifically block translation of individual transcripts.
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In VitroPF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM.PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50 of 2 μM.PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+ toxicity. Cell Cytotoxicity Assay Cell Line:Rat bone marrow lineage (?) cell and CD34+ cell Concentration:0-20 μM Incubation Time:72 h Result:Showed cytotoxicity with IC50 values of 2.9 μM and 2.7 μM against rat Lin(?) and human CD34+, respectively.
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In VivoPF-06446846 reduces circulating PCSK9 and total plasma cholesterol levels in vivo without obvious toxicity. Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, five per group; 6–8 wk old at initiation of dosing)Dosage:5, 15, and 50 mg/kg Administration:Oral administration, daily, 14 days Result:Reduced plasma PCSK9, total plasma cholesterol, and LDL-C (low-density lipoprotein cholesterol) in a dose-dependent manner without obvious toxicity.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorPCSK9
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Research Area——
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Indication——
Chemical Information
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CAS Number1632250-49-7
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Formula Weight433.9
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Molecular FormulaC22H20ClN7O
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Purity>98% (HPLC)
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Solubility——
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SMILESClc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Lintner N G , Mcclure K F , Donna P , et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain[J]. PLoS Biology, 2017, 15(3):e2001882-.
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