Zaurategrast ethyl ester
Based on 1 Customer Validation
Zaurategrast ethyl ester (CDP323), the ethyl ester proagent of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders.
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- Reinheit: 99.21%
- CAS. Nr.: 455264-30-9
- Formel: C28H29BrN4O3
- Molecular Weight:549.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
α4β1/α4β7 integrin[1]
Zaurategrast ethyl ester (CDP323), an ethyl ester prodrug of CT7758, shows some improvements in increasing mass transfer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 455264-30-9
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Appearance Solid
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Molecular Weight 549.46
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Formel C28H29BrN4O3
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Color Yellow to reddish brown
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SMILES
O=C(OCC)[C@H](CC1=CC=C(NC2=NC=CC3=C2C=NC=C3)C=C1)NC4=C(Br)C(C45CCCCC5)=O
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Synonyms
CDP323; UCB1184197
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 150 mg/mL (273.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Chanteux H, et al. Cross-Species Differences in the Preclinical Pharmacokinetics of CT7758, an α4β1/α4β7 Integrin Antagonist. Drug Metab Dispos. 2015 Sep;43(9):1381-91. [Content Brief]
[2]. Davenport RJ, et al. Alpha4-integrin antagonism--an effective approach for the treatment of inflammatory diseases? Drug Discov Today. 2007 Jul;12(13-14):569-76. [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 | 1.8200 mL | 9.0998 mL | 18.1997 mL | 45.4992 mL |
| 5 mM | 0.3640 mL | 1.8200 mL | 3.6399 mL | 9.0998 mL | |
| 10 mM | 0.1820 mL | 0.9100 mL | 1.8200 mL | 4.5499 mL | |
| 15 mM | 0.1213 mL | 0.6067 mL | 1.2133 mL | 3.0333 mL | |
| 20 mM | 0.0910 mL | 0.4550 mL | 0.9100 mL | 2.2750 mL | |
| 25 mM | 0.0728 mL | 0.3640 mL | 0.7280 mL | 1.8200 mL | |
| 30 mM | 0.0607 mL | 0.3033 mL | 0.6067 mL | 1.5166 mL | |
| 40 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1375 mL | |
| 50 mM | 0.0364 mL | 0.1820 mL | 0.3640 mL | 0.9100 mL | |
| 60 mM | 0.0303 mL | 0.1517 mL | 0.3033 mL | 0.7583 mL | |
| 80 mM | 0.0227 mL | 0.1137 mL | 0.2275 mL | 0.5687 mL | |
| 100 mM | 0.0182 mL | 0.0910 mL | 0.1820 mL | 0.4550 mL |
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