VUF11207 TFA
Based on 4 publication(s) in Google Scholar
VUF11207 TFA is a potent, selective, and orally active CXCR7/ACKR3 agonist (pKi = 8.1). VUF11207 TFA specifically activates CXCR7/ACKR3, recruits β-arrestin, and induces receptor internalization, while downregulating the pro-inflammatory, pro-osteoclastogenic, and tumor immunosuppressive signaling mediated by the CXCL12-CXCR4 axis. VUF11207 TFA can be used for research on glioblastoma, hypertension, and venous thrombosis.
For research use only. We do not sell to patients.
- CAS No.: 1492153-74-8
- Formula: C29H36F4N2O6
- Molecular Weight:584.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) VUF11207 TFA
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Biological Activity
Description
IC50 & Target
[1]|
CXCR7 8.1 (pKi) |
In Vitro
VUF11207 TFA reduces CXCL12 mRNA expression in human U87MG and Pt#3 cells and mouse GL261 glioblastoma cells[2].
VUF11207 TFA (500 nM) partially reverses CXCL12-induced ERK phosphorylation in glioblastoma cells, while it does not affect ERK phosphorylation by itself[2].
VUF11207 TFA (500 nM; 48 h) eliminates the promoting effect of GAMs on tumor cell growth in the co-culture system of glioblastoma cells and GAMs, and restores the cytotoxic killing activity of CD8+ T cells[2].
VUF11207 TFA (100 ng/mL; 5 days) inhibits RANKL (HY-P73388) and TNF-α (HY-P7090)-induced osteoclastogenesis in mouse bone marrow-derived osteoclast precursor cells in the presence of CXCL12[1].
VUF11207 TFA (100 ng/mL; 15-30 min) reduced CXCL12-enhanced Erk phosphorylation in mouse bone marrow-derived osteoclast precursors treated with RANKL or TNF-α[1].
VUF11207 TFA (0.5 μg/mL) promotes AngII (HY-13948)-induced expression of pro-inflammatory and pro-fibrotic factors in rat aortic adventitial fibroblasts (AFs) and exacerbates cell proliferation and migration[3].
VUF11207 TFA competitively displaces the fluorescent ligand in HEK293G cells overexpressing NLuc-ACKR3, specifically binding to the ACKR3 receptor[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Mouse bone marrow-derived osteoclast precursors
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Concentration:100 ng/mL
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Incubation Time:5 days
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Result:Decreased the number of TRAP-positive multinucleated osteoclasts and attenuated CXCL12-enhanced p-ERK levels without altering p38 or JNK.
In Vivo
VUF11207 TFA (5 mg/kg/d; i.g.; once daily; 14 days) significantly enhanced AngII-induced adventitial thickening and fibrosis in an AngII-induced hypertensive mouse model[3].
VUF11207 TFA (100 µg/day; s.c.; once daily; 5 days) significantly inhibited LPS (HY-D1056)-induced osteoclastogenesis and bone resorption in a mouse model, and reduced LPS-induced RANKL and TNF-α mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8-10 weeks old, 20-25 g, LPS-induced osteoclastogenesis and bone resorption model)[1]
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Dosage:100 µg/day
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Administration:s.c.; once daily; 5 days
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Result:Significantly reduced osteoclastogenesis compared with LPS alone.
Significantly lowered the number of TRAP-positive osteoclasts.
Significantly decreased TRAP and Cathepsin K mRNA expression levels.
Significantly reduced bone resorption area.
Significantly lowered RANKL and TNF-α mRNA levels.
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Animal Model:C57BL/6NCrlBltw (female, 8-12 weeks old)[2]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; from post-implantation day 7
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Result:Prolonged survival with median survival of 28 days for the VUF11207-anti-PD-L1 combination, compared to 18 days for VUF monotherapy, 20 days for anti-PD-L1 monotherapy, and 19 days for control.
Reduced tumor size on post-implantation day 20.
Decreased CXCL12 and PD-L1 expression, particularly PD-L1 in glioblastoma-associated macrophages (GAMs).
Attenuated phosphorylated ERK expression.
Increased proportion of CD8+ T cells in tumor tissues.
Achieved long-term survival in 4 of 9 mice when combined with anti-PD-L1 and control antibody, whereas all mice succumbed within 27 days when combined with anti-PD-L1 and anti-CD8β antibody.
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Animal Model:C57/B6 wild-type (WT) (male, ten weeks old, AngII-induced hypertension)[3]
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Dosage:5 mg/kg/d
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Administration:i.g.; once daily; 14 days
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Result:Strikingly aggravated aortic adventitial thickness, fibrosis, and collagen deposition in AngII-induced hypertensive mice.
Chemical Information
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CAS No. 1492153-74-8
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Molecular Weight 584.60
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Formula C29H36F4N2O6
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SMILES
O=C(N(C/C(C)=C/C1=CC=CC=C1F)CCC2N(C)CCC2)C3=CC(OC)=C(OC)C(OC)=C3.FC(C(O)=O)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
Cell Death Dis
CXCR7 activation evokes the anti-PD-L1 antibody against glioblastoma by remodeling CXCL12-mediated immunity. [Abstract]2024 Jun 19;15(6):434. PMID: 38898023 -
Cell Mol Life Sci
Crosstalk between purinergic receptor P2Y11 and chemokine receptor CXCR7 is regulated by CXCR4 in human macrophages. [Abstract]2024 Mar 13;81(1):132. PMID: 38472446 -
Protocols
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
[1]. Nugraha AP, et al. C‑X‑C receptor 7 agonist acts as a C‑X‑C motif chemokine ligand 12 inhibitor to ameliorate osteoclastogenesis and bone resorption. Molecular medicine reports. 2022 Mar;25(3):78. [Content Brief]
[2]. Liu CC, et al. CXCR7 activation evokes the anti-PD-L1 antibody against glioblastoma by remodeling CXCL12-mediated immunity. Cell death & disease. 2024 Jun 19;15(6):434. [Content Brief]
[5]. Aslan JE. A platelet lipid switch that slows clotting. Blood. 2026 Sep 10;148(11):1379-80.
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)