RANKL-IN-1 formate
Based on 1 Customer Validation
RANKL-IN-1 formate is a selective receptor activator of nuclear factor-κB ligand inhibitor ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 formate exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1 formate binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 formate can be used for the research of metabolic disease, such as osteoporosis.
For research use only. We do not sell to patients.
- Purity: 99.74%
- Formula: C41H57N5O3
- Molecular Weight:667.92
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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MMP-9 |
RANKL-IN-1 (Compound 19u) (50-400 nM, 4 days) formate shows no significant cytotoxicity in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) formate inhibits RANKL-induced osteoclastogenesis without affecting osteoblast differentiation in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) formate reduces RANKL-induced ROS levels and inhibits bone resorption in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) formate inhibits the expression of proteins associated with RANKL-induced osteoclast differentiation in RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:50, 100, 200 and 400 nM
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Incubation Time:4 days
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Result:Decreased the size of the F-actin ring.
Reduced ROS levels.
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Cell Line:RAW264.7 cells
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Concentration:50, 100, 200 and 400 nM
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Incubation Time:4 days
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Result:Downregulated the protein expression of TRAF6 and phosphorylation of p65, p38, ERK and JNK.
Downregulated the activity of the c-Fos/NFATc1 signaling and inhibited the expression of CTSK and MMP-9.
RANKL-IN-1 (0.5-2 mg/kg, p.o., every 2 days for 11 weeks) formate prevents systemic bone loss in ovariectomy-induced osteoporosis mice models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zebrafish osteoporosis models[1]
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Dosage:0.313, 0.625 and 1.25 μg/mL
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Administration:96 h
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Result:Increased zebrafish skull bone mass.
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Animal Model:Ovariectomy-induced osteoporosis mice models[1]
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Dosage:0.5, 1 and 2 mg/kg
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Administration:Orally administration, every 2 days for 11 weeks
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Result:Increased the bone mineral density, bone volume fraction, trabecular number and the trabecular thickness.
Reduced the trabecular separation and expanded the marrow cavity and trabecular spacing.
Reduced total cholesterol and triglyceride levels and increased high-density lipoprotein cholesterol levels.
Had no significant changes in ALT, AST and BUN levels.
Chemical Information
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Appearance Solid
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Molecular Weight 667.92
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Formula C41H57N5O3
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Color White to off-white
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SMILES
OC=O.[H][C@@]12C[C@@](C(N3CCC(CC3)N4CCNCC4)=O)(C)CC[C@]1(C)CC[C@@]5(C)[C@@]2(C)CC=C6C7=CC8=NC=CN=C8C(C)=C7C=C[C@@]56C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 12.5 mg/mL (18.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4972 mL | 7.4859 mL | 14.9719 mL | 37.4296 mL |
| 5 mM | 0.2994 mL | 1.4972 mL | 2.9944 mL | 7.4859 mL | |
| 10 mM | 0.1497 mL | 0.7486 mL | 1.4972 mL | 3.7430 mL | |
| 15 mM | 0.0998 mL | 0.4991 mL | 0.9981 mL | 2.4953 mL |
RANKL-IN-1 formate Related Classifications
HY-175703A Related Classifications
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