BIBP3226
目录号 : KCM11747 CAS No. : 159013-54-4 纯度 : ≥98%
BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y (K = 1.1 nM). It is selective for Y over Y, Y, and Y receptors (Ks = >1,000 nM for all). It also binds to neuropeptide FF receptor 1 (NPFF1) and NPFF2 (Ks = 108 and 79 nM, respectively) and reverses NPFF-induced inhibition of forskolin-induced cAMP accumulation in CHO cells expressing human NPFF2 in a concentration-dependent manner. BIBP3226 inhibits NPY-induced increases in perfusion pressure in isolated rat kidney but not the NPY-induced twitch response in isolated rat vas deferens (ICs = 26 and >10,000 nM, respectively). BIBP3226 inhibits NPY-induced increases in blood pressure in pithed rats (ED = 0.11 mg/kg). It also inhibits NPFF-induced hypothermia in mice when administered intracerebroventricularly (i.c.v.) at a dose of 5 nmol.
规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock

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生物活性

BIBP3226 is a potent and selective neuropeptide Y Y1 and neuropeptide FF receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 displays anxiogenic-like effect.

体内研究

BIBP3226 (0.5, 5 μg; i.c.v.; male Wistar rats) induces an anxiogenic-like effect at the higher dose.

分子式
C27H31N5O3
分子量
473.57
CAS号
159013-54-4
中文名称
N-[(1R)-4-[(氨基亚胺甲基)氨基]-1-[[[(4-羟基苯基)甲基]氨基]羰基]丁基]-alpha-苯基苯乙酰胺
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro:

DMSO : 100 mg/mL (211.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1116 mL 10.5581 mL 21.1162 mL
5 mM 0.4223 mL 2.1116 mL 4.2232 mL
10 mM 0.2112 mL 1.0558 mL 2.1116 mL
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂:10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.28 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO → 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.28 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。

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