| 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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| 100mg |
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| Other Sizes |
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VUF11207 fumarate is a novel, selective and highly potent agonist of CXCR7 (pKi of 8.1) , inducing the recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
| Targets |
CXCR7 ( pKi = 8.1 )
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|---|---|
| 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.
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| 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.
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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. |
| 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 |
| References |
|
| Molecular Formula |
C31H39FN2O8
|
|---|---|
| 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
|
| Complexity |
780
|
| Defined Atom Stereocenter Count |
0
|
| 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
|
| InChi Key |
MTPOECCHJLVVGO-FDULSSLPSA-N
|
| 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+
|
| 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
|
| 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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