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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-Asivatrep
Asivatrep

Chemical Structure : Asivatrep

CAS No.: 1005168-10-4

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Asivatrep (PAC-14028;PAC14028)

货号: PC-43202Not For Human Use, Lab Use Only.

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.

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10 mg ￥4280 In stock
25 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
Asivatrep 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.
Asivatrep also attenuates dermatitis-associated barrier damages in Df and OXZ models.

物理化学性质&存储条件

分子量 491.4747
分子式 C21H22F5N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 28 mg/mL
Chemical Name/SMILES

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

参考文献

1. Yun JW, et al. J Dermatol Sci. 2011 Apr;62(1):8-15.

2. Yun JW, et al. J Invest Dermatol. 2011 Jul;131(7):1576-9.

3. Lim KM, et al. Arch Pharm Res. 2012 Mar;35(3):393-6.

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