1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. 5-HT Receptor nAChR
  3. Tropisetron Hydrochloride

Tropisetron Hydrochloride  (Synonyms: 盐酸托烷司琼; SDZ-ICS-930)

目录号: HY-B0020 纯度: 99.97%
COA 产品使用指南 技术支持

Tropisetron Hydrochloride (SDZ-ICS-930) 是一种高效的神经保护剂,兼具 5-HT3 受体拮抗剂、钙调磷酸酶抑制剂以及 α7-nAChR 受体激动剂的特性,对 5-HT3 受体的 IC50 为 70.1 nM。Tropisetron Hydrochloride 具有抗炎特性和免疫调节功能,能够有效缓解化疗和术后相关症状。Tropisetron Hydrochloride 可减轻 Ab (HY-P4867) 诱导的海马神经炎症。

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Tropisetron Hydrochloride Chemical Structure

Tropisetron Hydrochloride Chemical Structure

CAS No. : 105826-92-4

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥425
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5 mg ¥387
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10 mg ¥472
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25 mg ¥684
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100 mg ¥1200
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Customer Review

Other Forms of Tropisetron Hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation[1][2][3][4].

IC50 & Target

5-HT3 Receptor

70.1 nM (IC50)

5-HT3 Receptor

 

α7-nAChR

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Oocyte EC50
10 nM
Compound: Tropisetron ICS-205-930
Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
[PMID: 15050614]
体外研究
(In Vitro)

Tropisetron Hydrochloride (1-1000 nM,1 h) 对猪视网膜神经节细胞 RGCs 中谷氨酸诱导的兴奋性毒性具有神经保护作用,EC50 为 62 nM[1]
Tropisetron Hydrochloride (100 nM,1 h) 在 RGCs 中对 pAkt 水平没有明显的影响,但显著降低与兴奋性毒性相关的 p38 MAPK 水平[1]
Tropisetron Hydrochloride (1 nM-10 mM,4 天)在小脑颗粒神经元 CGNs 中,抑制钙调磷酸酶活性[2]
Tropisetron Hydrochloride (1 nM-10 mM,4 天) 对 CGNs 细胞活力无影响[2]
Tropisetron Hydrochloride (10nM-10 μM,4 天) 在 CGNs 细胞中抑制钙调磷酸酶活性,提高 CB1 的表达,并降低 cAMP 含量[2]

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

Cell Viability Assay[1][2]

Cell Line: Pig RGCs induced by glutamate[1]; CGNs[2]
Concentration: 1, 10, 50, 100, 1000 nM; 1, 10, 100, 1000, 10000, 100000, 1000000 nM
Incubation Time: 1 h; 4 days
Result: Increased RGCs cell survival rate.
Had no effect on CGNs cell vitality at 1nM-10mM; higher doses reduced cell vitality.

Western Blot Analysis[2]

Cell Line: CGNs (rat)
Concentration: 100 nM, 1 μM, 10 μM
Incubation Time: 4 days
Result: Inhibited the activity of calcineurin, increased the expression of CB1, and reduced cAMP levels.

Real Time qPCR[2]

Cell Line: CGNs (rat)
Concentration: 100 nM, 1 μM, 10 μM
Incubation Time: 4 days
Result: Inhibited the activity of calcineurin, increased the expression of CB1, and reduced cAMP levels.
体内研究
(In Vivo)

Tropisetron Hydrochloride (5 mg/kg,腹腔注射,每日一次,32 天) 在自身免疫性脑脊髓炎 (EAE) 小鼠体内有免疫调节功能[3]
Tropisetron Hydrochloride (1 μg,脑室注射,单次剂量) 逆转了大鼠认知缺陷,通过 5-HT3 受体依赖和独立途径在体内保护抗 Ab (HY-P4867) 诱导的神经毒性[4]

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

Animal Model: Beta-amyloid (Ab) rat model of AD[4]
Dosage: 1 μg, single dose
Administration: Intracerebroventricular injection (ICV)
Result: Increased in TNF-a, COX-2, iNOS, NF-κB, active caspase 3, cytochrome c release and calcineurin phosphatase activity in the hippocampus.
Animal Model: Rxperimental autoimmune encephalomyelitis (EAE) mice induced by myelin oligodendrocyte glycoprotein peptide[3]
Dosage: 5 mg/kg, daily, 32 days
Administration: Intraperitoneal injection (i.p.)
Result: Improved the clinical symptoms of EAE, suppressed the infiltration of inflammatory cells in the central nervous system and demyelination, significantly reduced the number and extent of inflammatory lesions and demyelinated areas, decreased the quantity and function of effector T cells, and inhibited the production of pro-inflammatory cytokines IL-17, IL-6, and IL-2.
Clinical Trial
分子量

320.81

Formula

C17H21ClN2O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸托烷司琼

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 : 70 mg/mL (218.20 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)

H2O 中的溶解度 : ≥ 50 mg/mL (155.86 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1171 mL 15.5855 mL 31.1711 mL
5 mM 0.6234 mL 3.1171 mL 6.2342 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 120 mg/mL (374.05 mM); 澄清溶液; 超声助溶

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

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.97%

参考文献

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
H2O / DMSO 1 mM 3.1171 mL 15.5855 mL 31.1711 mL 77.9277 mL
5 mM 0.6234 mL 3.1171 mL 6.2342 mL 15.5855 mL
10 mM 0.3117 mL 1.5586 mL 3.1171 mL 7.7928 mL
15 mM 0.2078 mL 1.0390 mL 2.0781 mL 5.1952 mL
20 mM 0.1559 mL 0.7793 mL 1.5586 mL 3.8964 mL
25 mM 0.1247 mL 0.6234 mL 1.2468 mL 3.1171 mL
30 mM 0.1039 mL 0.5195 mL 1.0390 mL 2.5976 mL
40 mM 0.0779 mL 0.3896 mL 0.7793 mL 1.9482 mL
50 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5586 mL
60 mM 0.0520 mL 0.2598 mL 0.5195 mL 1.2988 mL
80 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9741 mL
100 mM 0.0312 mL 0.1559 mL 0.3117 mL 0.7793 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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.

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Tropisetron Hydrochloride
目录号:
HY-B0020
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