1. Cytoskeleton
  2. Integrin
  3. Firategrast

Firategrast (Synonyms: SB 683699)

Cat. No.: HY-14951 Purity: 99.88%
Handling Instructions

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.

For research use only. We do not sell to patients.

Firategrast Chemical Structure

Firategrast Chemical Structure

CAS No. : 402567-16-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 304 In-stock
Estimated Time of Arrival: December 31
5 mg USD 276 In-stock
Estimated Time of Arrival: December 31
10 mg USD 426 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

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Description

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity[1][2][3].

IC50 & Target[1][2]

α4β1

 

α4β7

 

In Vitro

Firategrast (0.1-10 µM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cells adhesion[2].
Firategrast is a potent Integrin α4β1 (VLA-4) antagonist (IC50=198 nM) at inhibiting the binding of soluble VCAM/Fc chimeric protein (sVCAM-1) to G2 acute lymphoblastic leukemia (ALL) cells. VLA-4 is composed of CD49d (α4) and CD29 (β1)[1][4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Firategrast (30 mg/kg/day in drinking water; starting 2 or 7 days post transplantation to 21 days) shows an overall reduction of leukemic cells in the spleen[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Wild-type C57BL/6J mice (8-12 weeks) with primary TCL1-tg splenocytes[3]
Dosage: 30 mg/kg
Administration: Drinking water; daily; starting 2 or 7 days post transplantation to 21 days
Result: Showed an overall reduction of leukemic cells in the spleen, accompanied by significant spleen weight reduction.
Clinical Trial
Molecular Weight

499.50

Formula

C₂₇H₂₇F₂NO₆

CAS No.
SMILES

O=C(O)[[email protected]@H](NC(C1=C(F)C=CC=C1F)=O)CC2=CC=C(C3=C(OC)C=C(COCC)C=C3OC)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (200.20 mM)

Ethanol : ≥ 50 mg/mL (100.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0020 mL 10.0100 mL 20.0200 mL
5 mM 0.4004 mL 2.0020 mL 4.0040 mL
10 mM 0.2002 mL 1.0010 mL 2.0020 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  1% SBE-beta-CD

    Solubility: 0.2 mg/mL (0.40 mM); Clear solution; Need ultrasonic and warming

*All of the co-solvents are provided by MCE.
References
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Keywords:

FirategrastSB 683699SB683699SB-683699IntegrinorallylymphocytesCNSmultiplesclerosisMSchroniclymphocyticleukemiaCLLVLA-4VCAMCD49dCD29Inhibitorinhibitorinhibit

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Product Name:
Firategrast
Cat. No.:
HY-14951
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