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Zaurategrast

Integrin inhibitor CAS# 455264-31-0

Zaurategrast

Catalog No. BCC2070----Order now to get a substantial discount!

Product Name & Size Price Stock
Zaurategrast:10mg $296.00 In stock
Zaurategrast:20mg $503.00 In stock
Zaurategrast:50mg $1184.00 In stock
Zaurategrast:100mg $2072.00 In stock
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Quality Control of Zaurategrast

Quality Control & MSDS

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Chemical structure

Zaurategrast

3D structure

Chemical Properties of Zaurategrast

Cas No. 455264-31-0 SDF Download SDF
PubChem ID 10186367 Appearance Powder
Formula C26H25BrN4O3 M.Wt 521.42
Type of Compound N/A Storage Desiccate at -20°C
Synonyms CDP323
Solubility DMSO : 100 mg/mL (191.79 mM; Need ultrasonic)
Chemical Name (2S)-2-[(2-bromo-3-oxospiro[3.5]non-1-en-1-yl)amino]-3-[4-(2,7-naphthyridin-1-ylamino)phenyl]propanoic acid
SMILES C1CCC2(CC1)C(=C(C2=O)Br)NC(CC3=CC=C(C=C3)NC4=NC=CC5=C4C=NC=C5)C(=O)O
Standard InChIKey KYHVWHYLKOHLKA-FQEVSTJZSA-N
Standard InChI InChI=1S/C26H25BrN4O3/c27-21-22(26(23(21)32)10-2-1-3-11-26)31-20(25(33)34)14-16-4-6-18(7-5-16)30-24-19-15-28-12-8-17(19)9-13-29-24/h4-9,12-13,15,20,31H,1-3,10-11,14H2,(H,29,30)(H,33,34)/t20-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Zaurategrast

DescriptionZaurategrast is a potent and oral-effective α4-integrin inhibitor.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].

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. [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.

Protocol

Animal Administration [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).

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. [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.

Zaurategrast Dilution Calculator

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Zaurategrast Molarity Calculator

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Preparing Stock Solutions of Zaurategrast

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9178 mL 9.5892 mL 19.1784 mL 38.3568 mL 47.946 mL
5 mM 0.3836 mL 1.9178 mL 3.8357 mL 7.6714 mL 9.5892 mL
10 mM 0.1918 mL 0.9589 mL 1.9178 mL 3.8357 mL 4.7946 mL
50 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.7671 mL 0.9589 mL
100 mM 0.0192 mL 0.0959 mL 0.1918 mL 0.3836 mL 0.4795 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Zaurategrast

Zaurategrast(CDP-323) is an integrin inhibitor.

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Description

Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.

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