GSK-1605786

Product Name: GSK-1605786
CAS No.: 698394-73-9
Chemical Name: GSK-1605786
Synonyms: CCX282-B;Vercirnon;GSK1605786;Traficet-EN;GSK-1605786;GSK 1605786;Vercirnon GSK1605786;Vercirnon, 10 mM in DMSO;4-(2-(4-tert-butylphenylsulfonamido)-5-chlorobenzoyl)pyridin-1(2H)-olate;4-(2-((4-(tert-Butyl)phenyl)sulfonamido)-5-chlorobenzoyl)pyridine 1-oxide
CBNumber: CB42668435
Molecular Formula: C22H21ClN2O4S
Formula Weight: 444.93
MOL File: 698394-73-9.mol

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GSK-1605786 Property

Boiling point:: 672.3±65.0 °C(Predicted)
Density: 1.29±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 25 mg/ml
form: A crystalline solid
pka: 7.07±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23131
Product name: Vercirnon
Packaging: 1mg
Price: $81
Updated: 2024/03/01

Cayman Chemical

Product number: 23131
Product name: Vercirnon
Packaging: 5mg
Price: $377
Updated: 2024/03/01

ChemScene

Product number: CS-4963
Product name: Vercirnon
Purity: 98.19%
Packaging: 5mg
Price: $420
Updated: 2021/12/16

AK Scientific

Product number: 6855CR
Product name: Vercirnon
Packaging: 5mg
Price: $517
Updated: 2021/12/16

ChemScene

Product number: CS-4963
Product name: Vercirnon
Purity: 98.19%
Packaging: 10mg
Price: $600
Updated: 2021/12/16

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GSK-1605786 Chemical Properties,Usage,Production

Description

Vercirnon is an orally bioavailable antagonist of chemokine receptor 9 (CCR9) with an IC₅₀ value of 5.4 nM for inhibition of CCL25-induced calcium mobilization in Molt-4 cells. It is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC₅₀s = >10 μM for all). It also inhibits CCL25-induced Molt-4 chemotaxis in 0.1% BSA/HBSS and in 100% human AB serum (IC₅₀s = 3.5 and 33.4 nM, respectively), as well as chemotaxis of human T cells stimulated by retinoic acid (RA) and mouse and rat thymocytes. Vercirnon binds allosterically to the intracellular side of CCR9 and prevents G protein coupling.

Uses

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].

in vivo

Vercirnon (GSK-1605786) (10, 50 mg/kg; sc; twice daily; starting at 2 weeks of age until 12 weeks of age) improves the severity of intestinal inflammation in the TNFΔARE mouse model^[1].

Animal Model:	C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)^[1]
Dosage:	10, 50 mg/kg
Administration:	Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age
Result:	Resulted in complete protection from the severe inflammation associated with TNF- overexpression at 50 mg/kg. A similar protective effect was also noted with a lower dose.

IC 50

CCR9: 10 nM (IC₅₀)

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. DOI:10.1124/jpet.110.169714
[2] Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340. DOI:10.1155/2015/628340
[3] Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4. DOI:10.1016/j.bmcl.2015.06.046

GSK-1605786 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GSK-1605786 manufacturers

Career Henan Chemical Co

Product: Vercirnon 698394-73-9
Price: US $1.00/KG
Min. Order: 1g
Purity: Min98% HPLC
Supply Ability: g/kg /ton
Release date: 2019-12-20

698394-73-9, GSK-1605786Related Search:

GSK-1605786A

GSK 1605786

GSK1605786

GSK-1605786

Vercirnon

Vercirnon GSK1605786

4-(2-(4-tert-butylphenylsulfonamido)-5-chlorobenzoyl)pyridin-1(2H)-olate

Benzenesulfonamide, N-[4-chloro-2-[(1-oxido-4-pyridinyl)carbonyl]phenyl]-4-(1,1-dimethylethyl)-

CCX282-B

Traficet-EN

chemotaxis,CCR,bioavailable,Vercirnon,oral,GSK 1605786,inhibit,inflammatory,Inhibitor,bowel,GSK1605786,chemokine,CC chemokine receptor,disease

4-(2-((4-(tert-Butyl)phenyl)sulfonamido)-5-chlorobenzoyl)pyridine 1-oxide

N-[4-chloro-2-[(1-oxido-4-pyridinyl)carbonyl]phenyl]-4-(1,1-dimethylethyl)-benzenesulfonamide

Vercirnon, 10 mM in DMSO

698394-73-9