CP-664511 - CAS 379692-00-9
Catalog number: 379692-00-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H34N4O6
Molecular Weight:
522.59
COA:
Inquire
Targets:
Others
Description:
CP-664511 is a potent compound that is a alpha4beta1/vascular cell adhesion molecule-1 (VCAM-1) inhibitor which has therapeutic potential in treating allergic airway disease.
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
3-((1S)-1-(((3-methoxy-4-((((2-methylphenyl)amino)carbonyl)amino)phenyl)acetyl)amino)-3-methylbutyl)-5-Isoxazolepropanoic acid;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Alpha4bet1/VCAM-1 Inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
USEDUTJSKDZBGX-QHCPKHFHSA-N
InChI:
1S/C28H34N4O6/c1-17(2)13-23(24-16-20(38-32-24)10-12-27(34)35)29-26(33)15-19-9-11-22(25(14-19)37-4)31-28(36)30-21-8-6-5-7-18(21)3/h5-9,11,14,16-17,23H,10,12-13,15H2,1-4H3,(H,29,33)(H,34,35)(H2,30,31,36)/t23-/m0/s1
Canonical SMILES:
Cc1ccccc1NC(=O)Nc2ccc(cc2OC)CC(=O)N[C@@H](CC(C)C)c3cc(on3)CCC(=O)O
1.Pulmonary eosinophilia in a murine model of allergic inflammation is attenuated by small molecule alpha4beta1 antagonists.
Kudlacz E;Whitney C;Andresen C;Duplantier A;Beckius G;Chupak L;Klein A;Kraus K;Milici A J Pharmacol Exp Ther. 2002 May;301(2):747-52.
Inhibition of alpha4beta1/vascular cell adhesion molecule-1 (VCAM-1) interactions have therapeutic potential in treating allergic airway disease because of the importance of these adhesion molecules in the trafficking of eosinophils, lymphocytes, and monocytes. We examined several small molecule inhibitors of alpha4beta1/VCAM-1 interactions with in vitro potencies (IC(50) values) ranging from 0.52 nM (CP-664511; 3-[3-(1-[2-[3-methoxy-4-(3-O-tolyl-ureido)phenyl]-acetylamino]-3-methyl-butyl)isoxazol-5-yl]-propionic acid) to 38.5 nM (CP-609643; 3-[3-methyl-1-[2-[4-(3-O-tolyl-ureido)-phenyl]-acetylamino]-butyl)-isoxazol-5-yl]-propionic acid). The same compounds were evaluated in vivo using a murine model of ovalbumin-induced pulmonary eosinophilia. In this model, systemic administration of antibodies against alpha4 reduced bronchoalveolar lavage (BAL) eosinophilia approximately 60%. Small molecule alpha4beta1 antagonists were administered by intratracheal instillation and demonstrated dose-dependent inhibition of BAL eosinophil numbers and achieved a maximum inhibition of approximately 60%. In general, the rank order of potency for these compounds in vitro was consistent with that observed in vivo, which confirms that their efficacy is likely via blockade of alpha4beta1/VCAM-1 interactions.
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