SB 218795

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SB 218795

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:

174635-53-1

SB 218795 是一种有效的选择性非肽NK3受体拮抗剂，对hNK3的K_i值为 13 nM。SB 218795 对 hNK3 的选择性分别比 hNK2 和 hNK1 高 90 倍和 7000 倍。SB 218795 可以抑制 NK3 受体介导的兔瞳孔收缩。

生物活性

SB 218795 is a potent and selective non-peptideNK3receptorantagonist, with aK_i13 nM forhNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibitNK3receptor-mediated pupillary constriction of the rabbit^[1]^[2].

IC₅₀& Target^[1]

hNK3

13 nM (Ki)

hNK2

1220 nM (Ki)

体外研究
(In Vitro)

SB 218795 (3-30 nM) antagonizes the contractile responses induced by the NK3 receptor agonist senktide in a surmountable and concentration-dependent manner^[2].
SB 218795 (0.3-3 μM) does not affect the contractile responses of the NK3 receptor agonist [MePhe7]-NKB in the rabbit iris sphincter muscle^[2].

体内研究
(In Vivo)

SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%^[2].

分子量

396.44

Formula

C₂₅H₂₀N₂O₃

CAS 号

174635-53-1

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.