Basic information Safety Supplier Related

PAC-14028

Basic information Safety Supplier Related

PAC-14028 Basic information

Product Name:
PAC-14028
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)-
  • Asivatrep (PAC-14028)
  • Xanthine Impurity 8
CAS:
1005168-10-4
MF:
C21H22F5N3O3S
MW:
491.47
Mol File:
1005168-10-4.mol
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PAC-14028 Chemical Properties

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
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PAC-14028 Usage And Synthesis

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

PAC-14028Supplier

Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Email
sales@rechemscience.com
Capot Chemical Co.,Ltd.
Tel
+86-（0）57185586718; +8613336195806
Email
sales@capot.com
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Email
sales@hzclap.com
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PAC-14028(1005168-10-4)Related Product Information