Firategrast (SB-683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist. Firategrast could reduce trafficking of lymphocytes into the central nervous system (CNS). This could decrease multiple sclerosis (MS) activity, but may compromise CNS immune surveillance. The integrins are a sort of transmembrane receptors that modulate the signal transduction from ECM to the cell. They are associated with a lot of diseases such as cancer, inflammation and thrombotic diseases.
Molecular Weight | 499.5 |
Formula | C27H27F2NO6 |
CAS Number | 402567-16-2 |
Solubility (25°C) | DMSO: ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Integrin Products |
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HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
LDV
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. |
Cyclo(RADfK)
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. |
Obtustatin
Obtustatin is a non-RGD disintegrin of 41 residues. |
Integrin Binding Peptide
Integrin Binding Peptide is derived by fibronectin. |
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