2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Ondansetron

Ondansetron  (Synonyms: 昂丹司琼; GR 38032; SN 307)

目录号: HY-B0002B 纯度: 99.37%
COA 产品使用指南

摩尔计算器

Ondansetron (GR 38032; SN 307) 为一种高度选择性的 5-HT3 受体拮抗剂，IC50 值为 103 pM。Ondansetron 通过拮抗位于周围和中枢神经局部的神经原的 5-HT receptor 而发挥止吐作用。Ondansetron 能抑制由化疗和放疗引起的恶心呕吐。Ondansetron 有口服生物活性。

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Ondansetron Chemical Structure

Ondansetron Chemical Structure

CAS No. : 99614-02-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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1 mg ￥156
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5 mg ￥312
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10 mg ￥500
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50 mg ￥800
In-stock
100 mg ￥1000
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ondansetron:

Ondansetron 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity[1][2][3][4][5][6][7][8].

IC50 & Target

5-HT3 Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 300 μM
Compound: ondansetron
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
0.03 μM
Compound: ondansetron
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
[PMID: 23241029]
HEK293 IC50
0.16 μM
Compound: ondansetron
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
0.16 μM
Compound: ondansetron
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
0.3 μM
Compound: ondansetron
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
0.4 μM
Compound: Ondansetron
Inhibition of human ERG expressed in HEK cells by patch clamp technique
Inhibition of human ERG expressed in HEK cells by patch clamp technique
[PMID: 20889341]
HEK293 IC50
1.7 μM
Compound: ondansetron
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
17.4 μM
Compound: ondansetron
Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
20.4 μM
Compound: Ondansetrone
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
MDCK-II IC50
< 0.01 μM
Compound: ondansetron
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
[PMID: 23241029]
Oocyte IC50
0.09 nM
Compound: 3
Antagonist activity at human 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method
Antagonist activity at human 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method
[PMID: 21486038]
Oocyte IC50
0.16 nM
Compound: 3
Antagonist activity at rat 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method
Antagonist activity at rat 5HT3A receptor expressed in xenopus oocytes assessed as inhibition of 5HT-induced effect by electrophysiological method
[PMID: 21486038]
体内研究
(In Vivo)

Ondansetron (GR 38032；SN 307) (2.4-6 mg/kg；腹腔注射；15 天六次) 在小鼠中 TD50 值为 3.7±0.6 mg/ kg，LD50 为 4.6±0.5 mg/kg[4]。
Ondansetron (8 mg/kg；腹腔注射；1 次) 联合 Olanzapine (HY-14541) 在预防 NSCLC 患者的 CINV 方面具有更好的效果，特别是对于后期患者[7]。
Ondansetron (2 mg/kg；腹腔注射；连续六天) 通过 5-HT3 受体表现出抗炎作用[8]。

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

Animal Model: NSCLC Patients Treated With Chemotherapy[7]
Dosage: 8 mg
Administration: Intraperitoneal Injection (i.p.)
Result: Showed TD50 and LD50 doses with 3.7±0.6 mg/kg and 4.6±0.5 mg/kg, respectively.
Animal Model: Male Swiss Mice with Colitis[8]
Dosage: 2 mg/kg
Administration: Intraperitoneal Injection (i.p.)
Result: Showed dramatic reduction in MPO activity and tumor necrosis factor-alpha, interleukin-6 and interleukin-1 beta.
Clinical Trial
分子量

293.36

Formula

C18H19N3O
CAS 号
性状

固体

颜色

White to off-white

中文名称

昂丹司琼；恩丹西酮；昂旦司琼；奥旦西隆；翁丹色创；翁丹西隆；翁旦斯隆；蒽丹西酮
运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 10 mg/mL (34.09 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 3.4088 mL 17.0439 mL 34.0878 mL
5 mM 0.6818 mL 3.4088 mL 6.8176 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 (protect from light)。-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: ≥ 1 mg/mL (3.41 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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: 1 mg/mL (3.41 mM); 悬浊液; 超声助溶

    此方案可获得 1 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 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。

    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 (protect from light)

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

Ondansetron 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 (protect from light)。-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 3.4088 mL 17.0439 mL 34.0878 mL 85.2195 mL
5 mM 0.6818 mL 3.4088 mL 6.8176 mL 17.0439 mL
10 mM 0.3409 mL 1.7044 mL 3.4088 mL 8.5220 mL
15 mM 0.2273 mL 1.1363 mL 2.2725 mL 5.6813 mL
20 mM 0.1704 mL 0.8522 mL 1.7044 mL 4.2610 mL
25 mM 0.1364 mL 0.6818 mL 1.3635 mL 3.4088 mL
30 mM 0.1136 mL 0.5681 mL 1.1363 mL 2.8407 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:

Ondansetron99614-02-5GR 38032 SN 307昂丹司琼恩丹西酮昂旦司琼奥旦西隆翁丹色创翁丹西隆翁旦斯隆蒽丹西酮GR38032GR-38032SN307SN 307SN-3075-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT Receptor AntagonistAntiemeticInhibitorinhibitorinhibit

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