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Firategrast

🥰Excellent
Catalog No. TQ0291Cas No. 402567-16-2
Alias SB 683699

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.

Firategrast

Firategrast

🥰Excellent
Purity: 99.16%
Catalog No. TQ0291Alias SB 683699Cas No. 402567-16-2
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 SizePriceAvailabilityQuantity
1 mg$39In Stock
5 mg$89In Stock
10 mg$143In Stock
25 mg$297In Stock
50 mg$488In Stock
100 mg$787In Stock
200 mg$1,070In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Purity:99.16%
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Product Introduction

Bioactivity
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]
AliasSB 683699
Chemical Properties
Molecular Weight499.5
FormulaC27H27F2NO6
Cas No.402567-16-2
SmilesCCOCc1cc(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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0020 mL10.0100 mL20.0200 mL100.1001 mL
5 mM0.4004 mL2.0020 mL4.0040 mL20.0200 mL
10 mM0.2002 mL1.0010 mL2.0020 mL10.0100 mL
20 mM0.1001 mL0.5005 mL1.0010 mL5.0050 mL
50 mM0.0400 mL0.2002 mL0.4004 mL2.0020 mL
DMSO
1mg5mg10mg50mg
100 mM0.0200 mL0.1001 mL0.2002 mL1.0010 mL

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