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Firategrast

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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

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Purity: 99.67%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
5 mg$89In StockIn Stock
10 mg$143In StockIn Stock
25 mg$297In StockIn Stock
50 mg$488In StockIn Stock
100 mg$787In StockIn Stock
200 mg$1,070-In Stock
1 mL x 10 mM (in DMSO)$98In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.67%
Appearance:Solid
Color:White
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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]
SynonymsSB 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/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
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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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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