Cart
sales@molnova.com
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 |
|
| 5MG | 176 | In Stock |
|
| 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
-
Product NamePF-06446846
-
NoteResearch use only, not for human use.
-
Brief DescriptionPF 06446846 is a potent and selective PCSK9 inhibitor PF-06446846 reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.
-
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.
-
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.
-
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.
-
Synonyms——
-
PathwayOthers
-
TargetOther Targets
-
RecptorPCSK9
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1632250-49-7
-
Formula Weight433.9
-
Molecular FormulaC22H20ClN7O
-
Purity>98% (HPLC)
-
Solubility——
-
SMILESClc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
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-.
molnova catalog
related products
-
Auraptene
Auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its C-7.
-
Amylin, amide, human
Amylin, a 37-amino acid polypeptide that is structurally related to calcitonin, is secreted from the B cells of the pancreas. Amylin has anoretic effects in rats. Amylin may be responsible for the etiology of insulin resistance of type II diabetes mellitus through its modulation of peripheral effects of insulin.
-
(-)-Hinokinin
(-)-Hinokinin has anti-genotoxic and anticarcinogenic potential.
