1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR

Vercirnon (Synonyms: GSK-1605786; CCX282-B)

Cat. No.: HY-15724 Purity: 98.04%
Handling Instructions

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

For research use only. We do not sell to patients.

Vercirnon Chemical Structure

Vercirnon Chemical Structure

CAS No. : 698394-73-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[3]

CCR9

10 nM (IC50)

In Vitro

Vercirnon (CCX282-B) 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].

In Vivo

Vercirnon (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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (56.19 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.2248 mL 1.1238 mL 2.2475 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

References
Cell Assay
[1]

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].

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

Animal Administration
[2]

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].

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

References
Molecular Weight

444.93

Formula

C₂₂H₂₁ClN₂O₄S

CAS No.

698394-73-9

SMILES

O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Vercirnon
Cat. No.:
HY-15724
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Vercirnon

Cat. No.: HY-15724