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GSK3008348

Chemical Structure : GSK3008348

CAS No.: 1629249-33-7

GSK3008348 (GSK-3008348)

Catalog No.: PC-60069Not For Human Use, Lab Use Only.

GSK3008348 is a potent, selective, RGD-mimetic integrin αvβ6 antagonist with KD value of 9.5 pM and 4.8 pM for αvβ6 in normal and IPF human lung tissue membrane preparations.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK3008348 is a potent, selective, RGD-mimetic integrin αvβ6 antagonist with KD value of 9.5 pM and 4.8 pM for αvβ6 in normal and IPF human lung tissue membrane preparations.
GSK3008348 exhibits a high affinity and a minimum of 26-fold selectivity for the αvβ6 integrin over the other RGD integrin family members.
GSK3008348 induces αvβ6 internalization and degradation in human lung epithelial cells.
GSK3008348 engages αvβ6, induces prolonged inhibition of TGFβ signaling and reduces lung collagen deposition and serum C3M, a marker of IPF disease progression, in murine bleomycin-induced lung fibrosis model.

Physicochemical Properties

M.Wt 487.636
Formula C29H37N5O2
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

(3S)-3-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-4-{(3S)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinyl}butanoic acid

References

1. John AE, et al. Nat Commun. 2020 Sep 16;11(1):4659.

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