Vercirnon sodium


Catalog No. Size PriceQuantity
M26261-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium 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: 886214-18-2

Molecular Weight: 466.91

Formula: C22H20ClN2NaO4S

Chemical Name: sodium 4-{[(1Z,6E)-6-[(4-tert-butylbenzenesulfonyl)imino]-3-chlorocyclohexa-2,4-dien-1-ylidene](oxido)methyl}pyridin-1-ium-1-olate

Smiles: [Na+].CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)/N=C1\C=CC(Cl)=C\C\1=C(\[O-])/C1=CC=[N+]([O-])C=C1

InChiKey: NKNHYMXTVRJZBC-YBZPVFAISA-M

InChi: InChI=1S/C22H21ClN2O4S.Na/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;/h4-14,26H,1-3H3;/q;+1/p-1/b21-19-,24-20+;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (214.17 mM; Need ultrasonic).

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) sodium inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. Vercirnon sodium inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon sodium inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC50 of 141 nM. Vercirnon sodium 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 (GSK1605786A) sodium (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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