2. Cytoskeleton
  3. Integrin
  4. Firategrast

Firategrast  (Synonyms: SB 683699)

Cat. No.: HY-14951 Purity: 99.62%
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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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
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Customer Review

Based on 6 publication(s) in Google Scholar

Firategrast Related Antibodies

Top Publications Citing Use of Products

View All Integrin Isoform Specific Products:

View All Isoforms
αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Firategrast Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@@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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (200.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  1% SBE-β-CD in Saline

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.62%

COA (249 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.0020 mL 10.0100 mL 20.0200 mL 50.0501 mL
5 mM 0.4004 mL 2.0020 mL 4.0040 mL 10.0100 mL
10 mM 0.2002 mL 1.0010 mL 2.0020 mL 5.0050 mL
15 mM 0.1335 mL 0.6673 mL 1.3347 mL 3.3367 mL
20 mM 0.1001 mL 0.5005 mL 1.0010 mL 2.5025 mL
25 mM 0.0801 mL 0.4004 mL 0.8008 mL 2.0020 mL
30 mM 0.0667 mL 0.3337 mL 0.6673 mL 1.6683 mL
40 mM 0.0501 mL 0.2503 mL 0.5005 mL 1.2513 mL
50 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0010 mL
60 mM 0.0334 mL 0.1668 mL 0.3337 mL 0.8342 mL
80 mM 0.0250 mL 0.1251 mL 0.2503 mL 0.6256 mL
100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
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Firategrast Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Firategrast402567-16-2SB 683699SB683699SB-683699IntegrinorallylymphocytesCNSmultiplesclerosisMSchroniclymphocyticleukemiaCLLVLA-4VCAMCD49dCD29Inhibitorinhibitorinhibit

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