Asivatrep

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Asivatrep (PAC-14028) 是一种有效的选择性 TRPV1 拮抗剂，对大鼠 DRG 神经元中辣椒素诱导的 Ca2+ 流入的 IC50 为 55 nM。

Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons, does not inhibit or activate other TRP channels such as hTRPV2, hTRPV3, hTRPM8 and hTRPA1; inhibits capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations, blocks capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice, also attenuates dermatitis-associated barrier damages in Df and OXZ models.Dermatitis Phase 3 Clinical.

Asivatrep (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. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain.

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. 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.

PAC-14028 | PAC14028

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Inflammation/Immunology

Dermatitis

1005168-10-4

491.4747

C21H22F5N3O3S

>98% (HPLC)

DMSO: ≥ 28 mg/mL

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

2-Propenamide, N-[(1R)-1-[3,5-difluoro-4-[(methylsulfonyl)amino]phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)-3-pyridinyl]-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years