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MedKoo Cat#: 530609 | Name: PF‑06446846
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

PF‑06446846
PF‑06446846
CAS#1632250-49-7 (free base)

Theoretical Analysis

MedKoo Cat#: 530609

Name: PF‑06446846

CAS#: 1632250-49-7 (free base)

Chemical Formula: C22H20ClN7O

Exact Mass: 433.1418

Molecular Weight: 433.90

Elemental Analysis: C, 60.90; H, 4.65; Cl, 8.17; N, 22.60; O, 3.69

Price and Availability

Size Price Availability Quantity
5mg USD 650.00 2 Weeks
25mg USD 1,850.00 2 Weeks
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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)

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
1: Aspnes GE, Coffey SB, Darout E, Dechert-Schmitt AM, Dullea RG, Kamlet AS, Limberakis C, Londregan AT, McClure KF, Menhaji-Klotz E, Piotrowski DW, Polivkova J, Raymer B, Ruggeri RB, Salatto CT, Tu M, Wei L, Xiao J. Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups. Bioorg Med Chem Lett. 2023 Aug 15;92:129394. doi: 10.1016/j.bmcl.2023.129394. Epub 2023 Jun 26. PMID: 37379958. 2: Zhang D, Li Q, Chen X, Nie X, Xue F, Xu W, Luan Y. An Injectable Hydrogel to Modulate T Cells for Cancer Immunotherapy. Small. 2022 Aug;18(32):e2202663. doi: 10.1002/smll.202202663. Epub 2022 Jul 17. PMID: 35843879. 3: Jacome Sanz D, Raivola J, Karvonen H, Arjama M, Barker H, Murumägi A, Ungureanu D. Evaluating Targeted Therapies in Ovarian Cancer Metabolism: Novel Role for PCSK9 and Second Generation mTOR Inhibitors. Cancers (Basel). 2021 Jul 24;13(15):3727. doi: 10.3390/cancers13153727. PMID: 34359627; PMCID: PMC8345177. 4: Li W, Chang ST, Ward FR, Cate JHD. Selective inhibition of human translation termination by a drug-like compound. Nat Commun. 2020 Oct 2;11(1):4941. doi: 10.1038/s41467-020-18765-2. PMID: 33009412; PMCID: PMC7532171. 5: Li W, Ward FR, McClure KF, Chang ST, Montabana E, Liras S, Dullea RG, Cate JHD. Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule. Nat Struct Mol Biol. 2019 Jun;26(6):501-509. doi: 10.1038/s41594-019-0236-8. Epub 2019 Jun 3. PMID: 31160784; PMCID: PMC6919564. 6: Liaud N, Horlbeck MA, Gilbert LA, Gjoni K, Weissman JS, Cate JHD. Cellular response to small molecules that selectively stall protein synthesis by the ribosome. PLoS Genet. 2019 Mar 15;15(3):e1008057. doi: 10.1371/journal.pgen.1008057. PMID: 30875366; PMCID: PMC6436758. 7: Disney MD. Inhibiting Translation One Protein at a Time. Trends Biochem Sci. 2017 Jun;42(6):412-413. doi: 10.1016/j.tibs.2017.04.008. Epub 2017 May 15. PMID: 28522328. 8: 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. Erratum in: PLoS Biol. 2018 Apr 17;16(4):e1002628. doi: 10.1371/journal.pbio.1002628. PMID: 28323820; PMCID: PMC5360235.