| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
At an IC50 of 6.8 nM, vercirnon (GSK-1605786) sodium inhibits primary CCR9-expressing cells' chemotaxis toward CCL25. Human T cells cultured with retinoic acid (RA) exhibit chemotaxis induced by CCL25, which is inhibited by vercirnonodium. Vercirnonodium has an IC50 of 141 nM and inhibits CCL25-mediated chemotaxis of RA cultured cells in 100% human AB serum. Vercirnonodium, with IC50 values of 6.9 nM and 1.3 nM, respectively, is a strong inhibitor of CCL25-induced chemotaxis in mouse and rat thymocytes [1].
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| ln Vivo |
Vercirnon (GSK1605786A) sodium (10, 50 mg/kg; subcutaneous injection; twice daily; starting at 2 weeks of age and up to 12 weeks of age) decreases the severity of intestinal inflammation in the TNFΔARE animal model [1].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (TNFΔARE terminal ileitis mouse model) [1]
Doses: 10, 50 mg/kg Route of Administration: subcutaneous injection; twice (two times) daily; starting at 2 weeks of age until 12 weeks of age Experimental Results: Severe inflammation associated with TNF overexpression was completely prevented at a dose of 50 mg/kg. Lower doses were similarly protective. |
| 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. |
| Molecular Formula |
C22H20CLN2NAO4S
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|---|---|
| Molecular Weight |
466.913
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| CAS # |
886214-18-2
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| Related CAS # |
Vercirnon;698394-73-9
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| SMILES |
ClC1C([H])=C([H])/C(/C(/C=1[H])=C(/C1C([H])=C([H])[N+](=C([H])C=1[H])[O-])\[O-])=N\S(C1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])(=O)=O.[Na+]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~214.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (10.71 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (10.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1417 mL | 10.7087 mL | 21.4174 mL | |
| 5 mM | 0.4283 mL | 2.1417 mL | 4.2835 mL | |
| 10 mM | 0.2142 mL | 1.0709 mL | 2.1417 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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