2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Pitolisant oxalate

Pitolisant oxalate  (Synonyms: Tiprolisant oxalate)

目录号: HY-12199A
产品使用指南

摩尔计算器

Pitolisant oxalate 是一种有效的选择性人重组 H3 受体选择性反向激动剂，Ki 为 0.16 nM。

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Pitolisant oxalate Chemical Structure

Pitolisant oxalate Chemical Structure

CAS No. : 362665-57-4

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Pitolisant oxalate 的其他形式现货产品:

Other Forms of Pitolisant oxalate:

Pitolisant oxalate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).

IC50 & Target

Ki: 0.16 nM (H3 receptor)[1]
EC50: 1.5 nM (H3 receptor)[1]
体外研究
(In Vitro)

On the stimulation of guanosine 5′-O-(3-[35S]thio)triphosphate binding to this receptor, Pitolisant (BF2.649) behaves as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity ~50% higher than that of ciproxifan. Pitolisant displaces [125I]iodoproxyfan binding from mouse brain cortical membranes with an IC50 value of 26.4±4.5 nM. Taking into account the Kd value of the radioligand (161±9 pM), the deduced Ki value for Pitolisant is 14±1 nM. Pitolisant displaces [125I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H3 receptor with an IC50 value of 4.2±0.2 nM. Taking into account the Kd value of the radioligand (50±4 pM), the deduced Ki value for Pitolisant is 2.7±0.5 nM. Pitolisant progressively reverses this response with a Hill coefficient close to unity and an IC50 value of 330±68 nM, leading to a Ki value of 17±4 nM. Pitolisant elicits a dose-dependent decrease of the basal-specific [35S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC50 value of 1.5±0.1 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Pitolisant oxalate 相关抗体:
体内研究
(In Vivo)

The administration of Pitolisantat a single dose of 10 mg/kg 30 min before a single dose of Olanzapine (2 mg/kg b.w.) also significantly affects immobility time in the FST. Subsequent administration of the aforementioned drug sequence in mice statistically significantly increases the duration of immobility in comparison to the time determined in the control group in the FST. It decreased locomotor activity as well. In contrast, the results obtained in subchronic treatment after fifteen administrations of both drugs (Pitolisant 10 mg/kg b.w., and after 30 min Olanzapine 2 mg/kg b.w., and again after 4 h Olanzapine 2 mg/kg b.w.) show that the administration of Pitolisant followed by that of Olanzapine equalized the locomotor activity in mice; in comparison to the level of motility in the control group, to which only Pitolisant is administered. More importantly, this combination of drugs significantly reduces immobility time to the level obtained in the control group in the forced swim test in mice [one-way ANOVA; F (3,20)=4.226,P=0.0181][2]. Rats given Pitolisant (10 mg/kg) during the conditioning phase stayed 502±94 s on the paired texture, a value not statistically different from that of controls, indicating that Pitolisant did not support place preference[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

385.88

Formula

C19H28ClNO5
CAS 号
性状

固体

颜色

Off-white to light yellow

中文名称

替洛利生草酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (129.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5915 mL 12.9574 mL 25.9148 mL
5 mM 0.5183 mL 2.5915 mL 5.1830 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (6.48 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.48 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

[35S]GTPγS binding assays are performed. CHO-K1 cells stably expressing the human H3 receptor (~400 fmol/mg protein) are homogenized in ice-cold buffer (50 mM Tris/HCl, pH 7.4). Homogenates are centrifuged twice (20,000g for 10 min at 4°C), and the final pellet is resuspended in 50 volumes of buffer. Membranes (550 μg of protein) are pretreated with adenosine deaminase (1 U/mL) and incubated for 60 min at 25°C with 0.1 nM [35S]GTPγS and the drugs to be tested in a final volume of 1 mL of assay buffer (50 mM Tris/HCl, 50 mM NaCl, 5 mM MgCl2, 10 μM GDP, and 0.02% bovine serum albumin, pH 7.4). The nonspecific binding is determined using 10 μM nonradioactive GTPγS. Incubations are stopped by rapid filtration under vacuum through GF/B glass fiber filters. After washing with ice-cold water, the radioactivity trapped on filters is counted by liquid scintillation spectrometry. A similar assay is used to assess competitive antagonism. In brief, membranes (10 μg of protein) of HEK-293 cells stably expressing the human H3 receptor (~600 fmol/mg protein) are preincubated in presence of Pitolisant in the buffer (50 mM Tris/HCl, pH 7.4, 10 mM MgCl2, 100 mM NaCl, and 10 μM GDP) in a 96-well microplate under gentle agitation at room temperature (19-20°C) for 30 min before the addition of 0.1 nM [35S]GTPγS (final volume 200 μL). The nonspecific binding is determined using a 10 μM concentration of nonradioactive GTPγS. After 30 min, incubations performed in triplicate are stopped by rapid filtration under vacuum on a Multiscreen MAFCOB50 microplate. Radioactivity trapped on filters is counted by liquid scintillation spectrometry[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Mice[2]
Adult female Albino Swiss mice weighing 20-22 g are used in the study. Olanzapine or Pitolisant are suspended in 1 % Tween 80. The compounds or vehicle are administered intraperitoneally (i.p.) 30 min prior to the acute experiment. In the Pitolisant+Olanzapine group, Pitolisant is administered 15 min before Olanzapine. Subchronic treatment is done at about 9:00 am (0.2 mL Tween to control group, Pitolisant-10 mg/kg b.w. to Pitolisant group, Olanzapine-2 mg/kg b.w. to Olanzapine group, Pitolisant-10 mg/kg b.w. and Olanzapine after 15 min-2 mg/kg b.w. to Pitolisant+Olanzapine group) and at about 1:00 pm (Olanzapine group and Pitolisant+Olanzapine group).
Rats[3]
Male Wistar rats (220-300 g) receive vehicle (methylcellulose 1%, p.o.), Pitolisant (10 mg/kg, p.o.) or D-amphetamine (2.5 mg/kg, i.p. in saline). Ninety minutes later, they are killed by decapitation and nucleus accumbens are dissected out, weighed, frozen in liquid nitrogen and stored at -80°C. Tissues are homogenized in 1 mL of a 0.4 N perchloric acid/2.7 mM EDTA solution. After centrifugation (8000 rpm, 20 min, 4°C), supernatants are analysed by HPLC coupled to electrochemical detection. Tissue concentrations of dopamine (DA), dihydroxyphenyl acetic acid (DOPAC) and homovanillic acid (HVA) are determined and the corresponding ratios (DOPAC/DA, HVA/DA) are calculated.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Pitolisant oxalate 相关分类

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5915 mL 12.9574 mL 25.9148 mL 64.7870 mL
5 mM 0.5183 mL 2.5915 mL 5.1830 mL 12.9574 mL
10 mM 0.2591 mL 1.2957 mL 2.5915 mL 6.4787 mL
15 mM 0.1728 mL 0.8638 mL 1.7277 mL 4.3191 mL
20 mM 0.1296 mL 0.6479 mL 1.2957 mL 3.2393 mL
25 mM 0.1037 mL 0.5183 mL 1.0366 mL 2.5915 mL
30 mM 0.0864 mL 0.4319 mL 0.8638 mL 2.1596 mL
40 mM 0.0648 mL 0.3239 mL 0.6479 mL 1.6197 mL
50 mM 0.0518 mL 0.2591 mL 0.5183 mL 1.2957 mL
60 mM 0.0432 mL 0.2160 mL 0.4319 mL 1.0798 mL
80 mM 0.0324 mL 0.1620 mL 0.3239 mL 0.8098 mL
100 mM 0.0259 mL 0.1296 mL 0.2591 mL 0.6479 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pitolisant362665-57-4Tiprolisant替洛利生草酸盐Histamine ReceptorInhibitorinhibitorinhibit

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