MEN 10207

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MEN 10207

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:

126050-12-2

MEN 10207 是一种选择性NK-2(Neurokinin Receptor) 速激肽受体拮抗剂。MEN 10207 在 NK-1、NK-2 和 NK-3 速激肽受体的三种单受体体外测定中的 pA₂值分别为 5.2、7.9 和 4.9。

生物活性

MEN 10207 is a selectiveNK-2 tachykinin receptor(Neurokinin Receptor) antagonist. MEN 10207 has pA₂values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively^[1]^[2].

IC₅₀& Target^[2]

Tachykinin NK₂Receptor

7.9 (pA2)

NK1

5.2 (pA2)

NK3

4.9 (pA2)

体外研究
(In Vitro)

In competitive radioligand binding assays, MEN 10207 (the IC₅₀ranges of 21-54 nM) has high affinity in bovine stomach membranes and SKLKB82#3 cells, a murine fibroblast cell line transfected with a cDNA encoding for the bovine NK2 receptor^[3].

体内研究
(In Vivo)

but not Substance P in a dose-dependent manner. And MEN 10207 also effectively blocks the long-term reflex facilitation to the gastrocnemius nerve stimulation^[1].

Animal Model:	Decerebrate, spinalized, unanesthetized Female Sprague-Dawley rats (250-280 g)^[1]
Dosage:	7 pmol/10 μL, 70 pmol/10 μL, 700 pmol/10 μL
Administration:	Intrathecal administration; once
Result:	Blocked the reflex facilitation to intrathecal Neurokinin A, but not Substance P in a dose-dependent manner.

分子量

1109.24

Formula

C₅₇H₆₈N₁₄O₁₀

CAS 号

126050-12-2

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.