1. Others GPCR/G Protein Neuronal Signaling
  2. Isotope-Labeled Compounds 5-HT Receptor
  3. Granisetron-d3

Granisetron-d3  (Synonyms: 格拉司琼-d3)

目录号: HY-132348S
产品使用指南 技术支持

Granisetron-d3 是 Granisetron 的氘代物。Granisetron (BRL 43694) 是5-HT3受体拮抗剂。

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Granisetron-d<sub>3</sub> Chemical Structure

Granisetron-d3 Chemical Structure

CAS No. : 1224925-64-7

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Other Forms of Granisetron-d3:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Granisetron-d3 is the deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.32 μM
Compound: Granisetron, Kutril
Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells by FLIPR assay
[PMID: 24128813]
HEK293 EC50
0.5 μM
Compound: Granisetron, Kutril
Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
Agonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells by FLIPR assay
[PMID: 24128813]
HEK293 IC50
311 μM
Compound: granisetron
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
4.3 μM
Compound: granisetron
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
5 μM
Compound: granisetron
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]
体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

分子量

315.43

Formula

C18H21D3N4O

CAS 号
非标记 CAS
中文名称

格拉司琼-d3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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Granisetron-d3
目录号:
HY-132348S
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