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Firategrast

Cat. No. M8939
Firategrast Structure
Synonym:

SB-683699; T-0047

Size Price Availability Quantity
5mg USD 145  USD145 In stock
10mg USD 225  USD225 In stock
25mg USD 450  USD450 In stock
50mg USD 740  USD740 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Halland N, et al. ACS Med Chem Lett. Small Macrocycles As Highly Active Integrin α2β1 Antagonists.

[2] Grove RA, et al. Eur J Neurol. Leukocyte counts in cerebrospinal fluid and blood following firategrast treatment in subjects with relapsing forms of multiple sclerosis.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Firategrast, SB-683699; T-0047 supplier, Integrin, inhibitors, activators


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