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.
Product information
CAS Number: 698394-73-9
Molecular Weight: 444.93
Formula: C22H21ClN2O4S
Chemical Name: 4-tert-butyl-N-[4-chloro-2-(1-oxo-1λ⁵-pyridine-4-carbonyl)phenyl]benzene-1-sulfonamide
Smiles: CC(C)(C)C1C=CC(=CC=1)S(=O)(=O)NC1=CC=C(Cl)C=C1C(=O)C1C=CN(=O)=CC=1
InChiKey: JRWROCIMSDXGOZ-UHFFFAOYSA-N
InChi: InChI=1S/C22H21ClN2O4S/c1-22(2,3)16-4-7-18(8-5-16)30(28,29)24-20-9-6-17(23)14-19(20)21(26)15-10-12-25(27)13-11-15/h4-14,24H,1-3H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 25 mg/mL (56.19 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Vercirnon (GSK-1605786) inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. Vercirnon inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC50 of 141 nM. Vercirnon is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC50 values of 6.9 nM and 1.3 nM, respectively.
In Vivo:
Vercirnon (GSK-1605786) (10, 50 mg/kg; s.c.; twice per day; starting at 2 weeks of age until 12 weeks of age) ameliorates the severity of intestinal inflammation in the TNFΔARE mouse model.
Products are for research use only. Not for human use.
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