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KPR-2579

(αR)-α-[Benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-benzeneacetamide

品牌
Sigma-Aldrich
CAS
1801742-41-5
货号
SML2411
规格纯度
≥98% (HPLC)
参考价格
798.09 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

生化/生理作用

KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs), stimulated by acetic acid (AA).
KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca2+ response in human/rat CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca2+ influx using hTRPA1, hTRPV1, or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects.

基本信息

经验(实验)分子式C23H20F2N2O2
分子量394.41

产品性质

测定≥98% (HPLC)
形式powder
旋光性[α]/D +124 to +136°, c = c=1 in chloroform-d
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度2-8℃
SMILES stringO=C(C1=CC=CC=C1)N([C@H](C)C2=CC(F)=CC(F)=C2)[C@H](C3=CC=CC=C3)C(N)=O

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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