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Firategrast

Cat. No. M8939
Firategrast Structure
Synonym:

SB-683699; T-0047

Size Price Availability Quantity
5mg USD 270 In stock
10mg USD 420 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 499.5
Formula C27H27F2NO6
CAS Number 402567-16-2
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Small Macrocycles As Highly Active Integrin α2β1 Antagonists.
Halland N, et al. ACS Med Chem Lett. 2014 Jan 10;5(2):193-8. PMID: 24900800.

Leukocyte counts in cerebrospinal fluid and blood following firategrast treatment in subjects with relapsing forms of multiple sclerosis.
Grove RA, et al. Eur J Neurol. 2013 Jul;20(7):1032-42. PMID: 23419064.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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