VUF 10460
目录号 : GC17585
A histamine H4 receptor agonist
Cas No.:1028327-66-3
Sample solution is provided at 25 µL, 10mM.
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VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
UF10460 binds to rat H3 and H4 receptor with pKi values of 5.75, and 7.46, respectively. VUF10460 displays approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor[1].
HCl-induced rat gastric lesions is significantly enhanced by the H4 receptor agonists VUF10460. This effect is not modified by H4 receptor antagonist JNJ7777120[1].
References:
[1]. Coruzzi G, 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.
Animal experiment: | Rats: VUF10460 is dissolved in 100% DMSO. Gastric lesions are induced in 24 h fasted rats by a single intragastric administration of 0.6 N HCl (5mL/kg volume). Drugs under study are administered subcutaneously 30 min before HCl. Rats are randomly divided to receive single doses (10 and/or 30 mg/kg) of immethridine, methimepip, immepip, VUF8430, VUF10460 or the vehicle, in a 1 mL/kg volume[1]. |
References: [1]. Coruzzi G, 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. | |
| Cas No. | 1028327-66-3 | SDF | |
| 化学名 | 4-(4-methylpiperazin-1-yl)-6-phenylpyrimidin-2(1H)-imine | ||
| Canonical SMILES | CN1CCN(C(C=C(N2)C3=CC=CC=C3)=NC2=N)CC1 | ||
| 分子式 | C15H19N5 | 分子量 | 269.34 |
| 溶解度 | DMSO: 100mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7128 mL | 18.5639 mL | 37.1278 mL |
| 5 mM | 0.7426 mL | 3.7128 mL | 7.4256 mL |
| 10 mM | 0.3713 mL | 1.8564 mL | 3.7128 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet