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Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $39 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $143 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $488 | In Stock | |
100 mg | $787 | In Stock | |
200 mg | $1,070 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
Description | Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid. |
Targets&IC50 | α4β1 (VLA-4):198 nM |
In vitro | Firategrast inhibiting the binding of soluble VCAM/Fc chimeric protein (sVCAM-1) to G2 acute lymphoblastic leukemia (ALL) cells.[2][5] Firategrast (0.1-10 µM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cell adhesion.[3] |
In vivo | Firategrast was administered at a dose of 30 mg/kg/day in drinking water, starting either 2 or 7 days after transplantation and continuing for 21 days. This treatment resulted in a significant decrease in leukemic cells present in the spleen.[4] |
Alias | SB 683699 |
Molecular Weight | 499.5 |
Formula | C27H27F2NO6 |
Cas No. | 402567-16-2 |
Smiles | CCOCc1cc(OC)c(c(OC)c1)-c1ccc(C[C@H](NC(=O)c2c(F)cccc2F)C(O)=O)cc1 |
Relative Density. | 1.261 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (180.2 mM) Ethanol: 45.0 mg/mL (90.1 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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