RANKL-IN-1
RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis.
For research use only. We do not sell to patients.
- CAS No.: 3108878-05-0
- Formula: C40H55N5O
- Molecular Weight:621.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 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) shows no significant cytotoxicity in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) inhibits RANKL-induced osteoclastogenesis without affecting osteoblast differentiation in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) reduces RANKL-induced ROS levels and inhibits bone resorption in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) 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.
| Species | Dose | Route | AUC0-t | AUC0-∞ | T1/2 | Tmax | Cmax | CL | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 5.529 mg·h/L | 5.814 mg·h/L | 18.981 h | 0.043 h | 3.012 mg/L | 1.748 L/h/kg | 12.394 h | 16.831 h | / |
| Mice[1] | 20 mg/kg | i.g. | 5.907 mg·h/L | 6.558 mg·h/L | 22.658 h | 6.000 h | 0.232 mg/L | / | 20.522 h | 29.128 h | 56.39 % |
| Rat[1] | 10 mg/kg | i.g. | 0.546 mg·h/L | 1.269 mg·h/L | 40.938 h | 5.600 h | 0.024 mg/L | / | 27.227 h | 61.837 h | 30.33 % |
| Rat[1] | 2 mg/kg | i.v. | 0.808 mg·h/L | 0.837 mg·h/L | 7.656 h | 0.017 h | 0.002 mg/L | 2.435 L/h/kg | 6.837 h | 8.410 h | / |
RANKL-IN-1 (0.5-2 mg/kg, p.o., every 2 days for 11 weeks) 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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CAS No. 3108878-05-0
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Molecular Weight 621.90
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Formula C40H55N5O
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SMILES
CC1=C(C2=CC3=NC=CN=C31)C=C[C@@]4(C2=CC[C@@]5([C@@]4(CC[C@@]6([C@H]5C[C@](C(N7CCC(CC7)N8CCNCC8)=O)(CC6)C)C)C)C)C
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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