KPR-5714 | TRPM8 antagonist | Probechem Biochemicals

Chemical Structure : KPR-5714

加入收藏

KPR-5714 (KPR5714)

货号: PC-72111Not For Human Use, Lab Use Only.

KPR-5714 (KPR5714) is a novel potent, selective TRPM8 antagonist with IC50 of 25.3 and 22.4 nM against hTRPM8 and rTRPM8, respectively.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

KPR-5714 (KPR5714) is a novel potent, selective TRPM8 antagonist with IC50 of 25.3 and 22.4 nM against hTRPM8 and rTRPM8, respectively.
KPR-5714 dispalys 400-fold against human TRPA1, TRPV1, and TRPV4, and does not show inhibitory effects for ASIC1a, ASIC3, Nav1.3, Nav1.5, Nav1.6, Nav1.7, and Nav1.8 (IC50 values >10 uM).
KPR-5714 (i.p.) inhibited the hyperactivity of mechanosensitive C-fibers of bladder afferents and dose-dependently increased the intercontraction interval shortened by intravesical instillation of acetic acid in anesthetized rats.
KPR-5714 (orally administered) dose-dependently increased the mean voided volume and decreased voiding frequency without affecting total voided volume in vivo.

物理化学性质&存储条件

分子量	474.42
分子式	C22H18F4N6O2
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	10 mM in DMSO
Chemical Name/SMILES	(R)-N-(3,3-difluoro-4-hydroxy-1-(2H-1,2,3-triazol-2-yl)butan-2-yl)-3-fluoro-2-(5-(4-fluorophenyl)-1H-pyrazol-3-yl)benzamide

参考文献

1. Nakanishi O, et al. J Pharmacol Exp Ther. 2020 May;373(2):239-247.

2. Aizawa N, et al. Eur J Pharmacol. 2021 May 15;899:173995.

KPR-5714 (KPR5714)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

KPR-5714 (KPR5714)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.