[CAS NO. 402567-16-2] Firategrast

Name: Firategrast
Brand: Arctom Scientific
SKU: AS941848

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PRODUCTS SPECIFICATIONS [402567-16-2]

Distributor

Catalog

AS941848

Brand

Arctom Scientific

CAS

402567-16-2

DESCRIPTION [402567-16-2]

Overview

MDL	MFCD19443754
Molecular Weight	499.50
Molecular Formula	C27H27F2NO6
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

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

4 Publications Citing Use of MCE

Summary

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

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 (IC ₅₀ =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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01416363	GlaxoSmithKline	Multiple Sclerosis, Relapsing-Remitting	May 20, 2011	Phase 1
NCT00395317	GlaxoSmithKline	Multiple Sclerosis	December 2006	Phase 2
NCT00469378	GlaxoSmithKline	Multiple Sclerosis	July 2007	Phase 2
NCT00097331	GlaxoSmithKline	Multiple Sclerosis, Relapsing-Remitting	September 2004	Phase 2

Appearance

Solid

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 available by MCE.