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| Cas No.: | 1005168-10-4 |
| Synonyms: | PAC14028; PAC 14028 |
| 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 |
| Formula: | C21H22F5N3O3S |
| M.Wt: | 491.47 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | PAC-14028 could prevent barrier damages, accelerate skin barrier recovery and suppress pruritus, showing a potential for the treatment of atopic dermatitis. It could suppress serum IgE increase, epidermal infiltration of inflammatory cells and mast cell degranulation associated with atopic dermatitis. PAC-14028 shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain.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 PAC-14028 is relatively well-absorbed through oral route. 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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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