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Vercirnon (Synonyms: CCX282-B, GSK1605786)

Katalog-Nr.GC18661

Vercirnon (GSK1605786A) ist ein oral bioverfÜgbarer, selektiver und potenter Antagonist von CCR9.

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Vercirnon Chemische Struktur

Cas No.: 698394-73-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Cells are harvested by centrifugation and resuspended in chemotaxis buffer consisting of HBSS with 0.1% BSA at a density of 107 cells/mL. For assays designed to determine Vercirnon potency in the presence of human serum, cells are resuspended in 100% human AB serum from pooled donors. Equal volumes of cell suspension and diluted Vercirnon are mixed and incubated for 10 min at room temperature. Twenty microliters of the mixture is transferred to the upper chamber of the chemotaxis chamber. After a 120-min incubation at 37°C, the assay is terminated by removal of cell drops from the top of the filter. Migration signal is determined by adding 5 μL of CyQUANT solution to each well in the lower chemotaxis chamber and measuring the intensity of fluorescence on a Spectrafluor Plus plate reader[1].

Animal experiment:

Mice[2]Female mdr1a−/− and wild-type FVB mice are used in the assay. CCX025, formulated in 1% hydroxypropyl methylcellulose, is dosed at 100 mg/kg s.c. once daily. Vercirnon, formulated in 5% Cremophor, is dosed at 50 mg/kg c.c. twice daily. During the course of the study, body weights and the incidence of diarrhea are recorded on a weekly basis. Any animals that exhibits weight loss of greater than 20% of their peak body weight are euthanized. Final body weights for any euthanized or dead animals are carried forward for data analysis. Diarrhea is scored on a 0-5 scale; when animals reach a score of ≥3, their diarrhea is constant and irreversible and is thus considered as established diarrhea[2].

References:

[1]. Walters MJ, et al. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther. 2010 Oct;335(1):61-9.
[2]. Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340.
[3]. Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4.

Background

Vercirnon (GSK-1605786) is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.

Vercirnon (GSK-1605786) is an orally bioavailable, selective, and potent antagonist of human CCR9. Vercirnon inhibits CCL25-induced calcium mobilization with an IC50 value of 5.4 ± 0.7 nM. Vercirnon is also a potent inhibitor of CCL25-induced Molt-4 chemotaxis with an IC50 of 3.5 ± 0.3 nM. Vercirnon shows inhibitory activity against Molt-4 migration with an IC50 of 33.4 ± 1.3 nM in 100% human AB serum. Moreover, Vercirnon suppresses the binding of [3H] CCX807 to Molt-4 cells with an IC50 of 6 nM. Vercirnon inhibits the chemotaxis of Baf-3/CCR9A cells as well as Baf-3/CCR9A cells with IC50s of 2.8 ± 1.1 nM and 2.6 ± 0.7 nM, respectively. Vercirnon potently inhibits CCL25-induced chemotaxis with an IC50 value of 6.8 ± 1.7 nM in buffer, and exhibits inhibition on RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum with an IC50 of 141 ± 13 nM[1].

Vercirnon (GSK-1605786) (10, 50 mg/kg twice daily) protects from the severe inflammation associated with TNF-α overexpression in the TNFΔARE Mouse Model. Vercirnon (50 mg/kg c.c. twice daily) blocks the colitis-associated weight loss inherent in the mdr1a−/− model, and also abrogates growth arrest in the colitis mdr1a −/− mice[2].

References:
[1]. Walters MJ, et al. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther. 2010 Oct;335(1):61-9.
[2]. Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340.
[3]. Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4.

Chemical Properties

Cas No. 698394-73-9 SDF
Überlieferungen CCX282-B, GSK1605786
Chemical Name N-[4-chloro-2-[(1-oxido-4-pyridinyl)carbonyl]phenyl]-4-(1,1-dimethylethyl)-benzenesulfonamide
Canonical SMILES O=C(C(C=C1)=CC=[N]1=O)C(C=C(Cl)C=C2)=C2N[S](=O)(C3=CC=C(C(C)(C)C)C=C3)=O
Formula C22H21ClN2O4S M.Wt 444.9
Löslichkeit DMSO: 25 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2477 mL 11.2385 mL 22.477 mL
5 mM 0.4495 mL 2.2477 mL 4.4954 mL
10 mM 0.2248 mL 1.1238 mL 2.2477 mL
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