| Identification | Back Directory | [Name]
PAC-14028 | [CAS]
1005168-10-4 | [Synonyms]
PAC-14028
PAC14028; PAC 14028
2-Propenamide, N-[(1R)-1-[3,5-difluoro-4-[(methylsulfonyl)amino]phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)-3-pyridinyl]-, (2E)- | [Molecular Formula]
C21H22F5N3O3S | [MDL Number]
MFCD28502100 | [MOL File]
1005168-10-4.mol | [Molecular Weight]
491.47 |
| Chemical Properties | Back Directory | [density ]
1.381±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 50 mg/mL (101.74 mM) | [form ]
Solid | [pka]
7.41±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist. | [in vivo]
Asivatrep (PAC-14028) shows a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively suggesting that Asivatrep (PAC-14028) is relatively well-absorbed through oral route[1]. Asivatrep (PAC-14028) could inhibit capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations. This potent TRPV1 antagonistic activity in keratinocytes is manifested in vivo as the blockade of capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice[3]. | [References]
[1] Park YH, et al. Oral and topical pharmacokinetic studies of a novel TRPV1 antagonist, PAC-14028 in rats and minipigs using liquid chromatography/tandem mass spectrometric method. J Pharm Biomed Anal. 2012 Mar 5;61:8-14. DOI:10.1016/j.jpba.2011.11.011
[2] Lim KM, et al. Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6. DOI:10.1007/s12272-012-0321-6
[3] Yun JW, et al. TRPV1 antagonist can suppress the atopic dermatitis-like symptoms by accelerating skin barrier recovery. J Dermatol Sci. 2011 Apr;62(1):8-15. DOI:10.1016/j.jdermsci.2010.10.014 |
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