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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $39 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $143 | In Stock | In Stock | |
| 25 mg | $297 | In Stock | In Stock | |
| 50 mg | $488 | In Stock | In Stock | |
| 100 mg | $787 | In Stock | In Stock | |
| 200 mg | $1,070 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock | 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] |
| Synonyms | 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (180.18 mM), Sonication is recommended. Ethanol: 45 mg/mL (90.09 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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