An integrin αVβ6 inhibitor
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GSK3008348

Item No. 43471

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(βS,3R)-β-[3-(3,5-dimethyl-(1H-pyrazol-1-(yl)phenyl]-3-([2-(5,6,7,8-(tetrahydro-(1,8-(naphthyridin-(2-yl)ethyl]-1-pyrrolidinebutanoic acid
CAS Number
1629249-33-7
Molecular Formula
C29H37N5O2
Formula Weight
487.6
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
OC(C[C@@H](C1=CC(N2N=C(C)C=C2C)=CC=C1)CN3C[C@H](CCC(N4)=CC=C5C4=NCCC5)CC3)=O
InChi Code
InChI=1S/C29H37N5O2/c1-20-15-21(2)34(32-20)27-7-3-5-24(16-27)25(17-28(35)36)19-33-14-12-22(18-33)8-10-26-11-9-23-6-4-13-30-29(23)31-26/h3,5,7,9,11,15-16,22,25H,4,6,8,10,12-14,17-19H2,1-2H3,(H,30,31)(H,35,36)/t22-,25-/m1/s1
InChi Key
ZMXBIIQMSGOIRZ-RCZVLFRGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $174

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    10 mg

    $251

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    25 mg

    $434

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    Product Description

    GSK3008348 is an integrin αVβ6 inhibitor (Ki = 0.01 nM).1 It is selective for integrin αVβ6 over integrins αVβ1, αVβ3, αVβ5, and αVβ8 (IC50s = 3.9, 50, 1,000, 126, and 16 nM, respectively, in cell adhesion assays). GSK3008348 induces internalization and degradation of integrin αVβ6 and reduces the phosphorylation of SMAD2 in normal human bronchial epithelial (NHBE) cells.2 Intranasal administration of GSK3008348 (3 mg/kg) decreases lung collagen levels in a mouse model of lung fibrosis induced by bleomycin (Item No. 13877).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Procopiou, P.A., Anderson, N.A., Barrett, J., et al. Discovery of (S)-3-(3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic acid, a nonpeptidic αvβ6 integrin inhibitor for the inhaled treatment of idiopathic pulmonary fibrosis. J. Med. Chem. 61(18), 8417-8443 (2018).

    2. John, A.E., Graves, R.H., Pun, K.T., et al. Translational pharmacology of an inhaled small molecule αvβ6 integrin inhibitor for idiopathic pulmonary fibrosis. Nat. Commun. 11(1), 4659 (2020).