GLPBio

GLPG0187

Catalog No.: GC19167Purity:>98.50%
COASDSData Sheet
GLPG0187 is a broad-spectrum integrin receptor antagonist that exhibits selectivity for various integrin receptors, with the following IC50 values: αVβ1 at 1.3nM, αVβ3 at 3.7nM, αVβ5 at 2.0nM, αVβ6 at 1.4nM, αVβ8 at 1.2nM, and α5β1 at 7.7nM.

Products are for research use only. Not for human use. We do not sell to patients.

GLPG0187
Cas No.: 1320346-97-1
1mgIn Stock
$82.00
1
5mgIn Stock
$226.00
1
10mgIn Stock
$308.00
1
50mgIn Stock
$750.00
1
100mgIn Stock
$1,024.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

No citations are currently available for this product. Below are selected publications citing GlpBio products.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Description

GLPG0187 is a broad-spectrum integrin receptor antagonist that exhibits selectivity for various integrin receptors, with the following IC50 values: αVβ1 at 1.3nM, αVβ3 at 3.7nM, αVβ5 at 2.0nM, αVβ6 at 1.4nM, αVβ8 at 1.2nM, and α5β1 at 7.7nM[1, 2]. GLPG0187 possesses anti-tumor activity, blocking the αvβ6 integrin receptor on cancer cells, locally preventing TGF-β activation, thereby reducing TGF-β signaling and immune evasion in cancer cells[3].

In vitro, GLPG0187 (20nM, 100nM, 200nM, 1µM) pretreatment of human small airway epithelial cells (HSAE) for 2h blocked SARS-CoV-2 delta and Omicron pseudovirus infection of airway epithelial cells in a dose-dependent manner[4]. Treatment of TALL-104 T lymphoblast cells with GLPG0187 (4µM) for 24h significantly enhanced the killing effect of TALL-104 T lymphoblast cells on HCT116 p53-null cells[5].

In vivo, GLPG0187 (100mg/kg) administered via intraperitoneal injection for 17 days in a mouse model of prostate cancer bone metastasis significantly reduced the number of tumor cells in the implanted metatarsal bones of the mice, significantly increased the number of osteoblasts, and significantly decreased microvessel density[6].

References:
[1] van der Horst G, van den Hoogen C, Buijs J T, et al. Targeting of αv-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer[J]. Neoplasia, 2011, 13(6): 516-IN9.
[2] Zhao-He L I, You Z, You-Xiang D, et al. Roles of integrin in tumor development and the target inhibitors[J]. Chinese journal of natural medicines, 2019, 17(4): 241-251.
[3] MacDonald W J, Verschleiser B, Carlsen L, et al. Broad spectrum integrin inhibitor GLPG-0187 bypasses immune evasion in colorectal cancer by TGF-β signaling mediated downregulation of PD-L1[J]. American Journal of Cancer Research, 2023, 13(7): 2938.
[4] Huntington K E, Carlsen L, So E Y, et al. Integrin/TGF-β1 inhibitor GLPG-0187 blocks SARS-CoV-2 delta and omicron pseudovirus infection of airway epithelial cells in vitro, which could attenuate disease severity[J]. Pharmaceuticals, 2022, 15(5): 618.
[5] Verschleiser B, MacDonald W, Carlsen L, et al. Pan-integrin inhibitor GLPG-0187 promotes T-cell killing of mismatch repair-deficient colorectal cancer cells by suppression of SMAD/TGF-β signaling[J]. American Journal of Cancer Research, 2023, 13(7): 2878.
[6] Reeves K J, Hurrell J E, Cecchini M, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187[J]. International journal of cancer, 2015, 136(7): 1731-1740.

Protocol

Cell experiment [1]:

Cell lines

Human small airway epithelial (HSAE)

Preparation Method

HSAE cells were pre-treated with 20nM, 100nM, 200nM, or 1µM GLPG0187 for 2h followed by spin infection with either a pseudovirus expressing the D614G spike protein variant or a VsVg positive control for 24h.

Reaction Conditions

20nM, 100nM, 200nM, 1µM; 2h

Applications

Pre-treatment with GLPG0187 resulted in the most significant decrease in pseudovirus infection by the Delta variant.
Animal experiment [2]:

Animal models

Server combined immune-deficiency (SCID) mouse

Preparation Method

A single murine metatarsal was engrafted into a dorsal skinfold chamber implanted on a SCID mouse. Fluorescently-labeled human prostate (PC3-GFP) cancer cells were administered via intracardiac (i.c) injection. Animals were administered GLPG0187 daily for 17 days (i.p 100mg/kg; n=20, dissolved in 2% DMSO in PBS) or vehicle control (2% DMSO in PBS n=20), commencing on the same day as tumour cell injection (day 7). Metatarsal recordings were taken every 48h for up to 4 weeks. At the end of treatment animals were culled (day 25). Tissue was harvested and processed for microCT, multiphoton analysis, histology and immunohistochemistry.

Dosage form

100mg/kg; 17 days; i.p.

Applications

GLPG0187 significantly reduced the number of tumour cells present in the implanted metatarsal from day 17 onwards. The number of osteoblasts was significantly increased in mice treated with GLPG0187. The microvessel density in the GLPG0187 treatment group was significantly lower compared to the control group.

References:
[1] Huntington K E, Carlsen L, So E Y, et al. Integrin/TGF-β1 inhibitor GLPG-0187 blocks SARS-CoV-2 delta and omicron pseudovirus infection of airway epithelial cells in vitro, which could attenuate disease severity[J]. Pharmaceuticals, 2022, 15(5): 618.
[2]Reeves K J, Hurrell J E, Cecchini M, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187[J]. International journal of cancer, 2015, 136(7): 1731-1740.

Product Documents

Purity:>98.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1320346-97-1
SMILES
O=C(O)[C@H](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC=C(OC)C=C5)=O
Molecular Formula
C29H37N7O5S
Molecular Weight
595.71
Solubility
DMSO : 15 mg/mL (25.18 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

Reviews

Review for GLPG0187

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%