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> Vercirnon [698394-73-9]

Vercirnon [698394-73-9]

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Cat# HY-15724-5mg

Size : 5mg

Brand : MedChemExpress

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Description

Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively[1].

IC50 & Target[3]

CCR9

10 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
2.6 nM
Compound: 25; CCX282-B, GSK-1605786
Antagonist activity at recombinant human CCR9B expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
Antagonist activity at recombinant human CCR9B expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
[PMID: 31703817]
BaF3 IC50
2.8 nM
Compound: 25; CCX282-B, GSK-1605786
Antagonist activity at recombinant human CCR9A expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
Antagonist activity at recombinant human CCR9A expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
[PMID: 31703817]
In Vitro

Vercirnon (GSK-1605786) 抑制表达 CCR9 的原代细胞向 CCL25 趋化，IC50 为 6.8 nM。Vercirnon 抑制 CCL25 诱导的视黄酸 (RA) 培养人 T 细胞的趋化性。Vercirnon 在 100% 人 AB 血清中抑制 RA 培养细胞 CCL25 介导的趋化性，IC50 为 141 nM。Vercirnon 是一种有效的 CCL25 诱导的小鼠和大鼠胸腺细胞趋化性抑制剂，IC50 值分别为 6.9 nM 和 1.3 nM[1]。

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

Vercirnon Related Antibodies

Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (56.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2475 mL 11.2377 mL 22.4754 mL
5 mM 0.4495 mL 2.2475 mL 4.4951 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Purity & Documentation
References

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