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MedKoo Cat#: 563632 | Name: PF-06424439 Mesylate
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Description:

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

PF-06424439 Mesylate is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Chemical Structure

PF-06424439 Mesylate
PF-06424439 Mesylate
CAS#1469284-79-4 (mesylate)

Theoretical Analysis

MedKoo Cat#: 563632

Name: PF-06424439 Mesylate

CAS#: 1469284-79-4 (mesylate)

Chemical Formula: C23H30ClN7O4S

Exact Mass:

Molecular Weight: 536.05

Elemental Analysis: C, 51.54; H, 5.64; Cl, 6.61; N, 18.29; O, 11.94; S, 5.98

Price and Availability

Size Price Availability Quantity
5mg USD 270.00
25mg USD 750.00 2 Weeks
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Related CAS #
1469284-78-3 (free base) 1469284-80-7 (HCl) 1469284-79-4 (mesylate)
Synonym
PF-06424439 Mesylate; PF 06424439 Mesylate; PF06424439 Mesylate;
IUPAC/Chemical Name
[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate
InChi Key
ZSTFDNQQOJUJFL-XFULWGLBSA-N
InChi Code
InChI=1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28;1-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27);1H3,(H,2,3,4)/t15-;/m1./s1
SMILES Code
O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6.CS(=O)(O)=O
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
>3 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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM.
In vitro activity:
MKC8866 treatment resulted in increased levels of several TAG species, and this effect was abolished by co-treatment with PF-06424439 (Fig. 4a, b). MKC8866 treatment also resulted in an accumulation of lipid droplets (LDs), the main storage compartments of TAGs in cells, as evidenced by increased uptake of Nile red in MKC8866-treated MDA-MB-231 and HCC1806 cells after 6 days (Fig. 4e-g). This accumulation of LDs was inhibited by treatment with PF-06424439 in MDA-MB-231 cells (Fig. 4e, f). Reference: Nat Commun. 2022 May 6;13(1):2493. https://pubmed.ncbi.nlm.nih.gov/35524156/
In vivo activity:
The preclinical candidate 9 (PF-06424439) demonstrated excellent ADMET properties and decreased circulating and hepatic lipids when orally administered to dyslipidemic rodent models. Reference: J Med Chem. 2015 Sep 24;58(18):7173-85. https://pubmed.ncbi.nlm.nih.gov/26349027/
Solvent mg/mL mM
Solubility
DMSO 130.5 243.51
Ethanol 88.0 164.16
Water 63.9 119.14
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 536.05 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
Formulation protocol:
1. Almanza A, Mnich K, Blomme A, Robinson CM, Rodriguez-Blanco G, Kierszniowska S, McGrath EP, Le Gallo M, Pilalis E, Swinnen JV, Chatziioannou A, Chevet E, Gorman AM, Samali A. Regulated IRE1α-dependent decay (RIDD)-mediated reprograming of lipid metabolism in cancer. Nat Commun. 2022 May 6;13(1):2493. doi: 10.1038/s41467-022-30159-0. PMID: 35524156; PMCID: PMC9076827. 2. Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. PMID: 26349027.
In vitro protocol:
1. Almanza A, Mnich K, Blomme A, Robinson CM, Rodriguez-Blanco G, Kierszniowska S, McGrath EP, Le Gallo M, Pilalis E, Swinnen JV, Chatziioannou A, Chevet E, Gorman AM, Samali A. Regulated IRE1α-dependent decay (RIDD)-mediated reprograming of lipid metabolism in cancer. Nat Commun. 2022 May 6;13(1):2493. doi: 10.1038/s41467-022-30159-0. PMID: 35524156; PMCID: PMC9076827.
In vivo protocol:
1. Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. PMID: 26349027.
1: Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. PubMed PMID: 26349027.