1. Cytoskeleton
  2. Integrin

Zaurategrast (Synonyms: CDP323)

Cat. No.: HY-70073 Purity: 98.55%
Data Sheet SDS Handling Instructions

Zaurategrast is a potent and oral-effective α4-integrin inhibitor.

For research use only. We do not sell to patients.
Zaurategrast Chemical Structure

Zaurategrast Chemical Structure

CAS No. : 455264-31-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $195 In-stock
5 mg $170 In-stock
10 mg $300 In-stock
25 mg $590 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

Zaurategrast is a potent and oral-effective α4-integrin inhibitor.

IC50 & Target

α4-integrin[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00484536 UCB Pharma|Biogen Multiple Sclerosis May 2007 Phase 2
NCT00726648 UCB Pharma|Biogen Relapsing Multiple Sclerosis July 2008 Phase 1|Phase 2
NCT00484536 UCB Pharma|Biogen Multiple Sclerosis May 2007 Phase 2
NCT00726648 UCB Pharma|Biogen Relapsing Multiple Sclerosis July 2008 Phase 1|Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9179 mL 9.5894 mL 19.1788 mL
5 mM 0.3836 mL 1.9179 mL 3.8358 mL
10 mM 0.1918 mL 0.9589 mL 1.9179 mL
Animal Administration
[3]

CDP323 is prepared as a 1% methylcellulose suspension containing 0.1% Tween 80 (Mice)[3].

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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

521.41

Formula

C₂₆H₂₅BrN₄O₃

CAS No.

455264-31-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Zaurategrast
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