Vercirnon [698394-73-9]
Cat# HY-15724-5mg
Size : 5mg
Brand : MedChemExpress
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.
For research use only. We do not sell to patients.
Vercirnon Chemical Structure
CAS No. : 698394-73-9
This product is a controlled substance and not for sale in your territory.
Based on 2 publication(s) in Google Scholar
Other Forms of Vercirnon:
- Vercirnon sodium In-stock
View All CCR Isoform Specific Products:
Description |
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]. |
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IC50 & Target[3] |
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In Vitro |
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. |
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In Vivo |
Vercirnon (GSK-1605786) (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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Clinical Trial |
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Molecular Weight |
444.93 |
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Formula |
C22H21ClN2O4S |
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CAS No. |
698394-73-9 |
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Appearance |
Solid |
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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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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
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. Preparing
Stock Solutions
View the 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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Purity & Documentation |
Purity: 98.26% |
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References |
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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 |
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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 Related Classifications
- GPCR/G Protein Immunology/Inflammation
- CCR