Zaurategrast |
| Catalog No.GC37960 |
Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 455264-31-0
Sample solution is provided at 25 µL, 10mM.
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Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor. α4-integrin[1]
CDP323 is an ethyl ester prodrug of CT7758, a potent carboxylic acid antagonist of α4β1 (very late antigen-4, VLA-4) and, to a lesser extent, α4β7 integrins. CDP323 is developed as a VLA-4 antagonist prodrug for the treatment of multiple sclerosis[2].
CDP323 is a potent and effective α4 inhibitor that is well tolerated at oral doses up to 1000 mg twice daily (bid). Relative to placebo, all dosages of Zaurategrast (CDP-323) significantly decreased the capacity of lymphocytes to bind vascular adhesion molecule-1 (VCAM-1) and the expression of α4-integrin on VCAM-1-binding cells. CDP323 at daily doses of 1000 or 2000 mg induced significant increases in total lymphocyte count and suppressed VCAM-1 binding by reducing unbound very late antigen-4 expression on lymphocytes[1]. After oral administration of CDP323, CT7758 is by far the most abundant circulating plasma component, peaking between 0.5 and 1.5 hours irrespective of the species. These data suggested that CDP323 is rapidly absorbed and efficiently hydrolyzed into CT7758. Plasma exposure of CT7758 showed a large species variability with dog>rat=mice>cynomolgus monkey. In the tested dose range of 25-50 mg/kg, the estimated oral bioavailability (i.e., based on intravenous administration of CT7758 and assuming linear PK) is 29, 27, 8, and 0.3% in mice, rat, dog, and cynomolgus monkey, respectively. CDP323 increased the absorption of CT7758 by 5- to 10-fold in rodents, whereas no significant increase is observed in dog and monkey[3].
[1]. Wolf C, et al. Pharmacodynamic consequences of administration of VLA-4 antagonist CDP323 to multiple sclerosis subjects: a randomized, double-blind phase 1/2 study. PLoS One. 2013;8(3):e58438. [2]. Chanteux H, et al. In Vitro Hydrolysis and Transesterification of CDP323, an α4β1/α4β7 Integrin Antagonist Ester Prodrug. Drug Metab Dispos. 2014 Jan;42(1):153-61. [3]. 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.
Animal experiment: | Mice[3]Male Wistar rats (250-320 g) and CD-1 mice (20-25 g), Non-naive male Beagle dogs weighing 10 kg, and non-naive male cynomolgus monkeys weighing 3 kg are used. For plasma pharmacokinetic studies, CT7758 is administered orally (5-10 mL/kg, 30 mg/kg) or intravenously (2 mL/kg, 3 mg/kg) as a solution in 10 mM phosphate buffer. CDP323 is administered orally as a 1% methylcellulose suspension containing 0.1% Tween 80 (same dosage volume as CT7758). Compounds are delivered to fasted animals with the food returned 4 hours postdose. Blood samples are collected at the designated time points. Plasma is prepared by centrifugation, collected, and stored at −20°C until analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS). |
References: [1]. Wolf C, et al. Pharmacodynamic consequences of administration of VLA-4 antagonist CDP323 to multiple sclerosis subjects: a randomized, double-blind phase 1/2 study. PLoS One. 2013;8(3):e58438. | |
| Cas No. | 455264-31-0 | SDF | |
| Canonical SMILES | O=C1C(Br)=C(C12CCCCC2)N[C@H](C(O)=O)CC3=CC=C(NC4=NC=CC5=CC=NC=C45)C=C3 | ||
| Formula | C26H25BrN4O3 | M.Wt | 521.41 |
| Solubility | DMSO: 100 mg/mL (191.79 mM) | Storage | Store at -20°C |
| 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. |
||
| 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 | 1.9179 mL | 9.5894 mL | 19.1788 mL |
| 5 mM | 383.6 μL | 1.9179 mL | 3.8358 mL |
| 10 mM | 191.8 μL | 958.9 μL | 1.9179 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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