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Firategrast

Catalog No. TQ0291 CAS 402567-16-2

Synonyms: SB 683699

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist.Firategrast reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.Firategrast is used in relapsing-remitting multiple sclerosis.Firategrast treatment is associated with a median cerebrospinal fluid associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts.

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Firategrast, CAS 402567-16-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 396.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.16%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist.Firategrast reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.Firategrast is used in relapsing-remitting multiple sclerosis.Firategrast treatment is associated with a median cerebrospinal fluid associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts.
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (180.2 mM)

Ethanol: 45.0 mg/mL (90.1 mM)

References and Literature

1. Grove RA, et al. Leukocyte counts in cerebrospinal fluid and blood following firategrast treatment in subjects with relapsing forms of multiple sclerosis. Eur J Neurol. 2013 Jul;20(7):1032-42. 2. Evbuomwan M O, et al. Generation and Characterization of Novel VLA-4 Inhibitors for Stem Cell Mobilization in Combination with a CXCR2 Agonist. Blood. 2017; 130: 3197. 3. Herman SE, et al. Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In Vivo. Clin Cancer Res. 2015;21(20):4642-4651. 4. Szenes E, et al. TCL1 transgenic mice as a model for CD49d-high chronic lymphocytic leukemia. Leukemia. 2020;34(9):2498-2502. 5. Rahimi H, et al. Aberrant regulation of the integrin very late antigen-4 in systemic lupus erythematosus. Lupus. 2013;22(3):297-306.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Bioactive Compounds Library Max Clinical Compound Library Bioactive Compound Library

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Keywords

Firategrast 402567-16-2 Cytoskeletal Signaling Integrin SB-683699 SB 683699 SB683699 inhibitor inhibit

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