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VUF10460 {[allProObj[0].p_purity_real_show]}

货号：A104244

VUF 10460 is a selective agonist of histamine H4 receptor with pKi of 8.22.

VUF10460 化学结构 CAS号：1028327-66-3
VUF10460 化学结构
CAS号：1028327-66-3
VUF10460 3D分子结构
CAS号：1028327-66-3
VUF10460 化学结构 CAS号：1028327-66-3
VUF10460 3D分子结构 CAS号：1028327-66-3
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VUF10460 纯度/质量文件 产品仅供科研

货号：A104244 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine 2HCl ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
Latrepirdine 2HCl ✔ GluR 99%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

VUF10460 生物活性

描述 Histamine H4 receptor expression was detected by immunohistochemistry in different areas of the gut and protective effects have been evidenced in various rodent models of gastric and intestinal damage. VUF10460 is a non-imidazole agonist of histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. VUF10460 displayed approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor. The ulcerogenic effect of immepip (a dual histamine H3/H4 receptor agonist) was mimicked by VUF10460 (10 mg/kg). Further, the aggravation of HCl-induced lesions observed after administration of VUF10460 was not significantly changed by JNJ7777120 (10 mg/kg; a histamine H4 receptor antagonist)[3].

VUF10460 参考文献

[1]Coruzzi G, Adami M, et al. Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur J Pharmacol. 2011 Nov 1;669(1-3):121-7.

[2]Cowart MD, Altenbach RJ, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem. 2008 Oct 23;51(20):6547-57.

[3]Selective Histamine H3 and H4 Receptor Agonists Exert Opposite Effects Against the Gastric Lesions Induced by HCl in the Rat Stomach

VUF10460 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.56mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL

VUF10460 技术信息

CAS号1028327-66-3
分子式C15H19N5
分子量 269.34
SMILES Code NC1=NC(C2=CC=CC=C2)=CC(N3CCN(C)CC3)=N1
MDL No. MFCD13187037
别名
运输蓝冰
InChI Key NIJGWJIOMPHDBP-UHFFFAOYSA-N
Pubchem ID 25129523
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: VUF10460 | 1028327-66-3 | VUF 10460 | VUF-10460 | H4 Receptor Agonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | VUF10460 纯度/质量文件 | VUF10460 亚型比较 | VUF10460 生物活性 | VUF10460 参考文献 | VUF10460 实验方案 | VUF10460 技术信息

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