WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H530609
CAS#: 1632250-49-7 (free base)
Description: PF‑06446846 is a PCSK9 inhibitor. PF-06446846 inhibits translation of PCSK9 by inducing the ribosome to stall around codon, mediated by the sequence of the nascent chain within the exit tunnel. 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.
Hodoodo Cat#: H530609
Name: PF‑06446846
CAS#: 1632250-49-7 (free base)
Chemical Formula: C22H20ClN7O
Exact Mass: 433.14
Molecular Weight: 433.900
Elemental Analysis: C, 60.90; H, 4.65; Cl, 8.17; N, 22.60; O, 3.69
Related CAS #: 1632250-49-7 (free base) 1632250-50-0 (HCl),
Synonym: PF‑06446846; PF 06446846; PF06446846;
IUPAC/Chemical Name: (R)-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)-N-(3-chloropyridin-2-yl)-N-(piperidin-3-yl)benzamide
InChi Key: FDTXHWQFIXYHCL-QGZVFWFLSA-N
InChi Code: InChI=1S/C22H20ClN7O/c23-18-5-2-12-25-20(18)29(17-4-1-11-24-14-17)22(31)15-7-9-16(10-8-15)30-21-19(27-28-30)6-3-13-26-21/h2-3,5-10,12-13,17,24H,1,4,11,14H2/t17-/m1/s1
SMILES Code: O=C(N(C1=NC=CC=C1Cl)[C@H]2CNCCC2)C3=CC=C(N4N=NC5=CC=CN=C54)C=C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the levels of plasma low-density lipoprotein cholesterol (LDL-C)
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 433.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Lintner NG, McClure KF, Petersen D, Londregan AT, Piotrowski DW, Wei L, Xiao
J, Bolt M, Loria PM, Maguire B, Geoghegan KF, Huang A, Rolph T, Liras S, Doudna
JA, Dullea RG, Cate JH. Selective stalling of human translation through
small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2017 Mar
21;15(3):e2001882. doi: 10.1371/journal.pbio.2001882. eCollection 2017 Mar.
PubMed PMID: 28323820; PubMed Central PMCID: PMC5360235.