| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
CXCR7 ( pKi = 8.1 )
CXCR7 (ACKR3) - high-potency agonist. |
|---|---|
| ln Vitro |
VUF11207 fumarate Fumarate (0.17 nM; 5 days) blocks RANKL- and TNF-α-induced osteoclastogenesis by blocking CXCL12 in osteoclast precursor cells [1]. Cell Viability Assay [1] Cell Line: Osteoclast Precursor Cells (RANKL- and TnF-α-induced) Concentration: 0.17 nM (100 ng/mL) Incubation Time: 5 Phosphorylation of erk to inhibit osteoclastogenesis [1]. Day results: showed inhibitory effect on CXCL12.
In vitro studies demonstrate that VUF11207 fumarate is a novel, selective, and high-potency agonist of CXCR7 (ACKR3) with a pKi of 8.1. The compound induces β-arrestin2 recruitment to the receptor with a pEC50 of 8.8 and promotes subsequent receptor internalization with a pEC50 of 7.9. These effects are characteristic of CXCR7 activation and are important for understanding the receptor's signaling mechanisms, which involve both G protein-dependent and β-arrestin-dependent pathways. CXCR7 is involved in cell migration, angiogenesis, and cancer progression, and VUF11207 fumarate serves as a valuable tool for studying these processes. |
| ln Vivo |
VUF11207 fumarate (100 μg/day; SC; once daily for 5 days) LPS-induced osteoclastogenesis, bone resorption, and RANKL and TNF-α production in cyclohexane [1]. : Male c57Bl/6J wild-type/WT mice (8-10 weeks old; 20-25 g; LPS induced) [1] Dose: 100 µg/day Administration: SC; once daily for 5 days Results: The number of osteoclasts was significantly reduced, and the expression levels of cathepsin K mRNA, ranKl and TnF-α mRNA were inhibited. Reduce LPS-induced bone resorption area.
In vivo studies on VUF11207 fumarate have demonstrated its value for research targeting bone metabolism and related pathologies. As a CXCR7 agonist, the compound is used to study the role of the CXCR7/CXCL12 axis in bone homeostasis, including the regulation of osteoblast and osteoclast function, bone remodeling, and skeletal development. The compound's high potency and selectivity for CXCR7 make it a key tool for investigating the therapeutic potential of CXCR7 modulation in bone diseases, cancer, and other pathologies involving CXCR7 signaling. Further studies are needed to fully characterize the compound's pharmacokinetic properties and efficacy in various disease models. |
| Enzyme Assay |
For receptor binding studies, competitive binding assays are performed using membrane preparations from cells expressing CXCR7. Membranes are incubated with a radiolabeled CXCR7 ligand and varying concentrations of VUF11207 fumarate. Bound radioactivity is separated by filtration and measured by scintillation counting. Binding affinity (pKi) is calculated from competition curves by non-linear regression analysis. For functional studies, β-arrestin2 recruitment assays are performed using cells expressing CXCR7 and a β-arrestin2 biosensor (e.g., BRET or PathHunter technology). Receptor internalization is assessed using fluorescence microscopy or flow cytometry to measure the loss of cell surface receptor staining following compound treatment.
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| Cell Assay |
Cell Line: Osteoclast precursor cells (RANKL‑ and TnF‑α‑induced)
Concentration: 0.17 nM (100 ng/mL) Incubation Time: 5 days Result: Showed inhibitory effect on CXCL12. Cellular assays for VUF11207 fumarate typically involve culturing cells that endogenously or recombinantly express CXCR7. Cells are treated with the compound at various concentrations, and receptor activation is assessed by measuring β-arrestin2 recruitment (using BRET, PathHunter, or similar assays), receptor internalization (by flow cytometry or microscopy), and downstream signaling pathways (such as ERK1/2 phosphorylation by Western blotting). Cell migration and invasion assays (wound healing, transwell) are performed to assess the functional consequences of CXCR7 activation. The compound's selectivity over other chemokine receptors is confirmed using similar assay formats. |
| Animal Protocol |
Male c57Bl/6J wild‑type/WT mice (8‑10‑week‑old; 20‑25 g; LPS-induced)
100 µg/day Subcutaneous injection; single daily for 5 days In vivo efficacy of VUF11207 fumarate is evaluated in animal models relevant to CXCR7 biology, including models of bone metabolism, cancer, and inflammatory diseases. For bone studies, mouse models of osteoporosis or bone fracture healing are used, with endpoints including bone mineral density measurement, micro-CT analysis of bone structure, and histomorphometric analysis. For cancer studies, xenograft or syngeneic mouse models are used to assess tumor growth, angiogenesis, and metastasis. Treatment is typically via intraperitoneal or oral administration. Pharmacokinetic studies are conducted to determine the compound's bioavailability and tissue distribution. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of VUF11207 fumarate have been characterized to support its use as a research tool. The compound's molecular weight of 586.65 and chemical properties influence its absorption, distribution, metabolism, and excretion (ADME) characteristics. Key PK parameters including half-life, clearance, volume of distribution, and oral bioavailability are determined using LC-MS/MS analysis of plasma and tissue samples following administration. The compound's ability to reach target tissues such as bone and tumors is important for its efficacy in in vivo studies. The fumarate salt form is used to improve the compound's solubility and stability.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of VUF11207 fumarate is typically conducted in parallel with efficacy studies in animal models. Standard toxicology assessments include acute toxicity studies to determine the maximum tolerated dose, observation of clinical signs and body weight changes, and histopathological examination of major organs following repeated dosing. As a CXCR7 agonist, potential effects on immune cell trafficking, angiogenesis, and development are carefully monitored. The compound's safety profile is established to define the therapeutic window for research applications. The compound is intended for laboratory research use only and is not approved for clinical administration.
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| References |
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| Additional Infomation |
VUF11207 fumarate is a research tool compound used for studying CXCR7 (ACKR3) signaling and its role in bone metabolism, cancer, cell migration, and development. The compound is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves selective and potent agonism of CXCR7, which triggers β-arrestin2 recruitment and receptor internalization, leading to modulation of downstream signaling pathways including ERK1/2 phosphorylation. This compound is valuable for investigating the therapeutic potential of CXCR7 modulation in bone diseases, cancer, and other pathologies, and for understanding the complex signaling mechanisms of this atypical chemokine receptor.
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| Molecular Formula |
C31H39FN2O8
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|---|---|
| Molecular Weight |
586.648372888565
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| Exact Mass |
586.27
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| CAS # |
1785665-61-3
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| Related CAS # |
1785665-61-3
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| PubChem CID |
90488970
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
42
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(=C\C1=CC=CC=C1F)/CN(CCC2CCCN2C)C(=O)C3=CC(=C(C(=C3)OC)OC)OC.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
MTPOECCHJLVVGO-FDULSSLPSA-N
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| InChi Code |
InChI=1S/C27H35FN2O4.C4H4O4/c1-19(15-20-9-6-7-11-23(20)28)18-30(14-12-22-10-8-13-29(22)2)27(31)21-16-24(32-3)26(34-5)25(17-21)33-4;5-3(6)1-2-4(7)8/h6-7,9,11,15-17,22H,8,10,12-14,18H2,1-5H3;1-2H,(H,5,6)(H,7,8)/b19-15+;2-1+
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| Chemical Name |
(E)-but-2-enedioic acid;N-[(E)-3-(2-fluorophenyl)-2-methylprop-2-enyl]-3,4,5-trimethoxy-N-[2-(1-methylpyrrolidin-2-yl)ethyl]benzamide
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| Synonyms |
VUF-11207 fumarate; VUF11207 fumarate; VUF 11207 fumarate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~170.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7046 mL | 8.5230 mL | 17.0459 mL | |
| 5 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL | |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7046 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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