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首页-小分子抑制剂&激动剂-GPCR-Adrenergic Receptor-L-771688
L-771688

Chemical Structure : L-771688

CAS No.: 200050-59-5

L-771688 (L-771,688, SNAP 6383)

货号: PC-20986Not For Human Use, Lab Use Only.

L-771688 (L-771,688, SNAP 6383) is a potent and selective alpha1A (α1A)-adrenoceptor antagonist with binding Ki of 0.13 nM to α1-adrenoceptors in human prostate tissue.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

L-771688 (L-771,688, SNAP 6383) is a potent and selective alpha1A (α1A)-adrenoceptor antagonist with binding Ki of 0.13 nM to α1-adrenoceptors in human prostate tissue.
L-771688 has Kd values of 71, 43 and 90 pM in cloned human α1A membranes, rat submaxillary gland and rat prostate membranes, respectively.
L-771,688 antagonizesnorepinephrine-induced inositol-phosphate responses in cloned human α1A-adrenoceptors, as well as phenylephrine or A-61603 induced contraction in isolated rat, dog and human prostate, human and monkey bladder neck and rat caudal artery with apparent Kb values of 0.02-0.28 nM.
The contraction of rat aorta induced by norepinephrine was resistant to L-771,688.

物理化学性质&存储条件

分子量 557.60
分子式 C28H33F2N5O5
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

O=C(C1=C(COC)NC(N(C(NCCCN2CCC(C3=NC=CC=C3)CC2)=O)[C@H]1C4=CC=C(F)C(F)=C4)=O)OC

参考文献

1. Chang RS, et al. Eur J Pharmacol. 2000 Dec 15;409(3):301-12.

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