Vercirnon
Based on 5 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.01%
- CAS 番号: 698394-73-9
- 分子式: C22H21ClN2O4S
- 分子量:444.93
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CCR9 10 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | EC50 |
2.8 nM
Compound: CCX-282
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Inhibition of chemotaxis in mouse BAF3 cells
Inhibition of chemotaxis in mouse BAF3 cells
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[PMID: 31266686] |
| BaF3 | IC50 |
2.6 nM
Compound: 25; CCX282-B, GSK-1605786
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Antagonist activity at recombinant human CCR9B expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
Antagonist activity at recombinant human CCR9B expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
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[PMID: 31703817] |
| BaF3 | IC50 |
2.8 nM
Compound: 25; CCX282-B, GSK-1605786
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Antagonist activity at recombinant human CCR9A expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
Antagonist activity at recombinant human CCR9A expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay
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[PMID: 31703817] |
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)[1]
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Dosage:10, 50 mg/kg
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Administration:Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 698394-73-9
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性状 Solid
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分子量 444.93
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分子式 C22H21ClN2O4S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O
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別名
GSK-1605786; CCX282-B; Traficet-EN
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Immunity
MAIT cells egress the thymus at several maturation stages with selective capacity to seed different tissues. [Abstract]2026 Jun 9;59(6):1512-1526.e5. PMID: 42025176 -
Nat Commun
TCF-1 and TOX regulate the memory formation of intestinal group 2 innate lymphoid cells in asthma. [Abstract]2024 Sep 8;15(1):7850. PMID: 39245681 -
Med
Intestinal barrier dysfunction plays an integral role in arthritis pathology and can be targeted to ameliorate disease. [Abstract]2021 Jul 9;2(7):864-883.e9. PMID: 34296202 -
ACS Pharmacol Transl Sci
Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. [Abstract]2024 Apr 18;7(5):1533-1545. PMID: 38751637 -
PeerJ
CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway. [Abstract]2022 Aug 19:10:e13844. PMID: 36003306
溶剤 & 溶解度
DMSO : ≥ 25 mg/mL (56.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340. [Content Brief]
[3]. Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2475 mL | 11.2377 mL | 22.4754 mL | 56.1886 mL |
| 5 mM | 0.4495 mL | 2.2475 mL | 4.4951 mL | 11.2377 mL | |
| 10 mM | 0.2248 mL | 1.1238 mL | 2.2475 mL | 5.6189 mL | |
| 15 mM | 0.1498 mL | 0.7492 mL | 1.4984 mL | 3.7459 mL | |
| 20 mM | 0.1124 mL | 0.5619 mL | 1.1238 mL | 2.8094 mL | |
| 25 mM | 0.0899 mL | 0.4495 mL | 0.8990 mL | 2.2475 mL | |
| 30 mM | 0.0749 mL | 0.3746 mL | 0.7492 mL | 1.8730 mL | |
| 40 mM | 0.0562 mL | 0.2809 mL | 0.5619 mL | 1.4047 mL | |
| 50 mM | 0.0450 mL | 0.2248 mL | 0.4495 mL | 1.1238 mL |
Vercirnon 関連分類
HY-15724 関連分類
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