DH97

立即咨询

DH97

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

220339-00-4

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议

产品介绍

DH97 是一种有效和选择性的MT₂褪黑激素受体拮抗剂，对人 MT₂的pK_i为 8.03。DH97 对人 MT2 的选择性比人 mt₁和非洲爪蟾 mel_1c受体亚型高 89 倍和 229 倍。DH97 可以抑制褪黑激素诱导的电诱发反应增强。

生物活性

DH97 is a potent and selective antagonist ofMT₂melatonin receptor, with apK_iof 8.03 for human MT₂. DH97 shows 89- and 229-fold selectivity for human MT₂over human mt₁andXenopusmel_1creceptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses^[1]^[2].

IC₅₀& Target^[1]

MT2

8.03 (pKi)

MT1

6.08 (pKi)

体外研究
(In Vitro)

DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) inXenopus laevismelanophores^[1].
DH97 has no agonist activity at concentrations up to 100 μM^[1].
DH97 (60 nM) significantly alteres the potency of melatonin in the rat tail artery at low concentrations of the MT2 selective ligands, with a pEC₅₀of 8.83^[2].
DH97 (5 μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT₂receptors^[2].

分子量

334.45

Formula

C₂₂H₂₆N₂O

CAS 号

220339-00-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.