Vercirnon sodium (Synonyms: GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium) |
| رقم الكتالوجGC61372 |
الصوديوم فيرسيرنون (GSK1605786A) هو مضاد حيوي متاح ، وانتقائي ، وفعال عن طريق الفم لـ CCR9
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 886214-18-2
Sample solution is provided at 25 µL, 10mM.
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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[1].
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[1].
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[1]. Animal Model: C57BL/6 mice (TNFδARE Mouse Model of Terminal Ileitis)[1]
[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.
| Cas No. | 886214-18-2 | SDF | |
| المرادفات | GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium | ||
| Canonical SMILES | O=S(C1=CC=C(C(C)(C)C)C=C1)([N-]C2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O.[Na+] | ||
| Formula | C22H20ClN2NaO4S | M.Wt | 466.91 |
| الذوبان | DMSO: 100 mg/mL (214.17 mM) | Storage | 4°C, stored under nitroge |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1417 mL | 10.7087 mL | 21.4174 mL |
| 5 mM | 428.3 μL | 2.1417 mL | 4.2835 mL |
| 10 mM | 214.2 μL | 1.0709 mL | 2.1417 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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