WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H562066
CAS#: 1467059-70-6
Description: PF-249, also known as PF-06685249, is a beta1-selective AMPK agonist. PF-06685249 is a potent AMPK activator. PF-06685249 exhibited robust activation of AMPK in rat kidneys as well as desirable oral absorption, low plasma clearance, and negligible renal clearance in preclinical species.
Hodoodo Cat#: H562066
Name: PF-249
CAS#: 1467059-70-6
Chemical Formula: C17H16ClN3O3
Exact Mass: 345.09
Molecular Weight: 345.780
Elemental Analysis: C, 59.05; H, 4.66; Cl, 10.25; N, 12.15; O, 13.88
Related CAS #: 1467059-70-6
Synonym: PF-249; PF 249; PF249; PF-06685249; PF-06685249; PF-06685249; PF-6685249; PF-6685249; PF-6685249;
IUPAC/Chemical Name: 6-Chloro-5-(6-(dimethylamino)-2-methoxypyridin-3-yl)-1H-indole-3-carboxylic acid
InChi Key: MJHBRTGGZYSCHJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H16ClN3O3/c1-21(2)15-5-4-9(16(20-15)24-3)10-6-11-12(17(22)23)8-19-14(11)7-13(10)18/h4-8,19H,1-3H3,(H,22,23)
SMILES Code: O=C(C1=CNC2=C1C=C(C3=CC=C(N(C)C)N=C3OC)C(Cl)=C2)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: >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:
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| In vitro activity: | |
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The following data is based on the product molecular weight 345.78 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: Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO, Tran JL, Jatkar A, Cialdea K, Esquejo RM, Meissen J, Calabrese MF, Cordes J, Moccia R, Tess D, Salatto CT, Coskran TM, Opsahl AC, Flynn D, Blatnik M, Li W, Kindt E, Foretz M, Viollet B, Ward J, Kurumbail RG, Kalgutkar AS, Wojtaszewski JFP, Cameron KO, Miller RA. Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice. Cell Metab. 2017 May 2;25(5):1147-1159.e10. doi: 10.1016/j.cmet.2017.04.010. PubMed PMID: 28467931.
2: Willows R, Navaratnam N, Lima A, Read J, Carling D. Effect of different γ-subunit isoforms on the regulation of AMPK. Biochem J. 2017 May 9;474(10):1741-1754. doi: 10.1042/BCJ20170046. PubMed PMID: 28302767; PubMed Central PMCID: PMC5423082.
3: Salatto CT, Miller RA, Cameron KO, Cokorinos E, Reyes A, Ward J, Calabrese MF, Kurumbail RG, Rajamohan F, Kalgutkar AS, Tess DA, Shavnya A, Genung NE, Edmonds DJ, Jatkar A, Maciejewski BS, Amaro M, Gandhok H, Monetti M, Cialdea K, Bollinger E, Kreeger JM, Coskran TM, Opsahl AC, Boucher GG, Birnbaum MJ, DaSilva-Jardine P, Rolph T. Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy. J Pharmacol Exp Ther. 2017 May;361(2):303-311. doi: 10.1124/jpet.116.237925. Epub 2017 Mar 13. PubMed PMID: 28289077.
