PAC 14028

• CAT Number: I008538
• CAS Number: 1005168-10-4
• Molecular Formula: C21H22F5N3O3S
• Molecular Weight: 491.47
• Purity: ≥95%
• Synonyms: PAC 14028; PAC-14028; PAC14028;(R,E)-N-(1-(3,5-difluoro-4-(methylsulfonamido)phenyl)ethyl)-3-(2-propyl-6-(trifluoromethyl)pyridin-3-yl)acrylamide
• Solubility: Soluble in DMSO
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: (E)-N-[(1R)-1-[3,5-difluoro-4-(methanesulfonamido)phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)pyridin-3-yl]prop-2-enamide
• InChI: InChI=1S/C21H22F5N3O3S/c1-4-5-17-13(6-8-18(28-17)21(24,25)26)7-9-19(30)27-12(2)14-10-15(22)20(16(23)11-14)29-33(3,31)32/h6-12,29H,4-5H2,1-3H3,(H,27,30)/b9-7+/t12-/m1/s1
• InChIKey: UKGJZDSUJSPAJL-YPUOHESYSA-N
• SMILES: O=C(N[C@@H](C1=CC(F)=C(NS(=O)(C)=O)C(F)=C1)C)/C=C/C2=CC=C(C(F)(F)F)N=C2CCC

PAC 14028(CAT: I008538) is described as a vanilloid VR1 receptor (TRPV1) antagonist. The transient receptor potential vanilloid 1 (TRPV1) receptor is involved in the perception of pain, as well as itch and inflammation. By acting as an antagonist of the TRPV1 receptor, PAC 14028 may have the potential to reduce itching (pruritus) and alleviate symptoms associated with conditions such as pruritus and acne. However, it’s important to note that further research and development would be necessary to fully understand its therapeutic applications and assess its efficacy and safety.

Reference

1:Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Lim KM, Park YH.Arch Pharm Res. 2012 Mar;35(3):393-6. doi: 10.1007/s12272-012-0321-6. PMID: 22477184
2:Oral and topical pharmacokinetic studies of a novel TRPV1 antagonist, PAC-14028 in rats and minipigs using liquid chromatography/tandem mass spectrometric method. Park YH, Joo KM, Woo BY, Son ED, Byun SY, Shin HJ, Lee KW, Park YH, Lim KM.J Pharm Biomed Anal. 2012 Mar 5;61:8-14. doi: 10.1016/j.jpba.2011.11.011. Epub 2011 Nov 17. PMID: 22169466