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MedKoo Cat#: 525976 | Name: PF-915275
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Description:

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

PF-915275 is a potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) PF-915275 inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC50 = 15 nM) and has antidiabetic activity in vivo.

Chemical Structure

PF-915275
PF-915275
CAS#857290-04-1

Theoretical Analysis

MedKoo Cat#: 525976

Name: PF-915275

CAS#: 857290-04-1

Chemical Formula: C18H14N4O2S

Exact Mass: 350.0837

Molecular Weight: 350.40

Elemental Analysis: C, 61.70; H, 4.03; N, 15.99; O, 9.13; S, 9.15

Price and Availability

Size Price Availability Quantity
10mg USD 325.00
50mg USD 885.00
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Related CAS #
No Data
Synonym
PF-915275; PF 915275; PF915275.
IUPAC/Chemical Name
N-(6-Aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide
InChi Key
ZESFDAKNYJQYKO-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H14N4O2S/c19-12-13-4-6-14(7-5-13)15-8-10-16(11-9-15)25(23,24)22-18-3-1-2-17(20)21-18/h1-11H,(H3,20,21,22)
SMILES Code
O=S(C1=CC=C(C2=CC=C(C#N)C=C2)C=C1)(NC3=NC(N)=CC=C3)=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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells).
In vitro activity:
Priming with NP (nonylphenol) significantly increased the PPARγ and FASN (p < 0.05, Fig. 6a, c) mRNA expression levels, whereas PF (PF-915275) treatment significantly decreased their mRNA expression levels (p < 0.05, Fig. 6a, c). In contrast, PF treatment significantly increased PPARα mRNA expression (p < 0.05, Fig. 6b), and priming with NP significantly decreased PPARα protein expression (p < 0.01, Fig. 6e), but PF significantly reversed this phenomenon (p < 0.05, Fig. 6e). Reference: BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. https://pubmed.ncbi.nlm.nih.gov/30021644/
In vivo activity:
In the rat model, PF915275 alleviated NP-induced effects by interfering with adipogenesis pathways, including enhancing PPARα expression, decreasing PPARγ expression, and reducing both 11β-HSD1 protein and mRNA expression levels. Additionally, PF915275 reduced the effects of the adrenal corticoid synthesis pathway by reducing StAR expression and 11β-hydroxylase and aldosterone synthase activities. Reference: BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. https://pubmed.ncbi.nlm.nih.gov/30021644/
Solvent mg/mL mM comments
Solubility
DMSO 33.0 94.24
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 350.40 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:
Chang LL, Wun WA, Wang PS. An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. doi: 10.1186/s40360-018-0235-0. PMID: 30021644; PMCID: PMC6052566.
In vitro protocol:
Chang LL, Wun WA, Wang PS. An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. doi: 10.1186/s40360-018-0235-0. PMID: 30021644; PMCID: PMC6052566.
In vivo protocol:
Chang LL, Wun WA, Wang PS. An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. doi: 10.1186/s40360-018-0235-0. PMID: 30021644; PMCID: PMC6052566.
1: Chang LL, Wun WA, Wang PS. An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol. 2018 Jul 18;19(1):45. doi: 10.1186/s40360-018-0235-0. PMID: 30021644; PMCID: PMC6052566. 2: Yang X, Hua W, Ryu S, Yates P, Chang C, Zhang H, Di L. 11β-Hydroxysteroid Dehydrogenase 1 Human Tissue Distribution, Selective Inhibitor, and Role in Doxorubicin Metabolism. Drug Metab Dispos. 2018 Jul;46(7):1023-1029. doi: 10.1124/dmd.118.081083. Epub 2018 Apr 19. PMID: 29674492. 3: Chang LL, Wun WS, Wang PS. Nonylphenol-induced hyperadrenalism can be reversed/alleviated by inhibiting of 11-β hydroxysteroid dehydrogenase type 1. Environ Toxicol Pharmacol. 2016 Jun;44:1-12. doi: 10.1016/j.etap.2016.03.019. Epub 2016 Mar 26. PMID: 27060500. 4: Zhao L, Pan Y, Peng K, Wang Z, Li J, Li D, Tong C, Wang Y, Liang G. Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice. J Mol Endocrinol. 2015 Oct;55(2):119-31. doi: 10.1530/JME-14-0268. Epub 2015 Jul 28. PMID: 26220348. 5: Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24. PMID: 23489629. 6: Dorniak P, Welsh TH Jr, Bazer FW, Spencer TE. Cortisol and interferon tau regulation of endometrial function and conceptus development in female sheep. Endocrinology. 2013 Feb;154(2):931-41. doi: 10.1210/en.2012-1909. Epub 2012 Dec 21. PMID: 23264615. 7: Lee SE, Kim JM, Jeong MK, Zouboulis CC, Lee SH. 11β-hydroxysteroid dehydrogenase type 1 is expressed in human sebaceous glands and regulates glucocorticoid-induced lipid synthesis and toll-like receptor 2 expression in SZ95 sebocytes. Br J Dermatol. 2013 Jan;168(1):47-55. doi: 10.1111/bjd.12009. PMID: 22897663. 8: Harno E, White A. Will treating diabetes with 11β-HSD1 inhibitors affect the HPA axis? Trends Endocrinol Metab. 2010 Oct;21(10):619-27. doi: 10.1016/j.tem.2010.06.004. Epub 2010 Jun 30. PMID: 20594868. 9: Siu M, Johnson TO, Wang Y, Nair SK, Taylor WD, Cripps SJ, Matthews JJ, Edwards MP, Pauly TA, Ermolieff J, Castro A, Hosea NA, LaPaglia A, Fanjul AN, Vogel JE. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7. doi: 10.1016/j.bmcl.2009.05.011. Epub 2009 May 7. PMID: 19473839. 10: Courtney R, Stewart PM, Toh M, Ndongo MN, Calle RA, Hirshberg B. Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor. J Clin Endocrinol Metab. 2008 Feb;93(2):550-6. doi: 10.1210/jc.2007-1912. Epub 2007 Nov 6. PMID: 17986636. 11: Bhat BG, Hosea N, Fanjul A, Herrera J, Chapman J, Thalacker F, Stewart PM, Rejto PA. Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino- pyridin-2-yl)-amide (PF-915275), an inhibitor of 11 -hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305. doi: 10.1124/jpet.107.128280. Epub 2007 Oct 5. PMID: 17921190.