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TBC3486

Chemical Structure : TBC3486

CAS No.: 247044-77-5

TBC3486 (TBC-3486;TBC 3486)

Catalog No.: PC-61261Not For Human Use, Lab Use Only.

TBC3486 is a potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TBC3486 is a potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM).
TBC3486 mimics VCAM-1 binding, preferentially inhibits the high-affinity form of the integrin α4, blocks integrin-dependent T-cell co-activation in vitro as well as proves to be efficacious in vivo at low doses in animal models of allergic inflammation.
TBC3486 dose-dependently inhibits adhesion of ALL cells, prolongs the survival of xenotolerant mice bearing human leukemia cells in vivo.

Physicochemical Properties

M.Wt 557.68
Formula C27H31N3O6S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-3-(benzo[d][1,3]dioxol-5-yl)-3-(3-((S)-1-(bis(thiophen-2-ylmethyl)amino)-1-oxohexan-2-yl)ureido)propanoic acid

References

1. Hsieh YT, et al. Leukemia. 2014 Oct;28(10):2101-4.

2. Vanderslice P, et al. Biochem Biophys Res Commun. 2010 Oct 1;400(4):619-24.

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