| Description |
sRANKL-IN-2 (Compound S3-05) is a selective and orally active soluble RANKL (sRANKL) inhibitor with an IC50 of 0.41 μM. sRANKL-IN-2 can be used for the research of osteoporosis[1].
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| Related Catalog |
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| Target |
soluble RANKL[1]
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| In Vitro |
sRANKL-IN-2 (Compound S3-05) (0.03-10 μM; 24 h) induces mature osteoclasts apoptosis and attenuates bone resorption in a dose-dependent manner[1]. sRANKL-IN-2 (0-10 μM; 14 days) increases cell proliferation and mineralization in mouse embryonic mesenchymal stem cell line C3H10T1/2 or human primary osteoblasts cells with osteogenic differentiation medium[1]. Apoptosis Analysis[1] Cell Line: Mature osteoclasts Concentration: 0.03, 0.1, 0.3, 1, 3 and 10 μM Incubation Time: 24 h Result: Significantly increased apoptosis of mature osteoclasts with an EC50 of 0.53 μM. Cell Proliferation Assay[1] Cell Line: C3H10T12 cells Concentration: 0.08, 0.28, 0.92, 3.03 and 10 μM Incubation Time: 14 days Result: Increased cell proliferation and mineralization in mouse embryonic mesenchymal stem cell line C3H10T1/2.
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| In Vivo |
sRANKL-IN-2 (Compound S3-05) (10 mg/kg/d; i.g.; 12 weeks) shows anti-osteoporosis activity in ovariectomy rats[1]. Animal Model: Female SD ovariectomy (OVX) rats[1] Dosage: 10 mg/kg/d Administration: Oral administraton, 12 weeks Result: Reduced bone loss, improved trabecular osteoporosis parameters, increased the bone volume / total volume (BV/TV). Animal Model: 28-week-old and 280 g∼370 g weight male SD (Sprague Dawley) rats[1] Dosage: 10 mg/kg Administration: Oral gavage (Pharmacokinetic Study) Result: The pharmacokinetic parameters of sRANKL-IN-2[1] sRANKL-IN-2 AUC (hr*μg/mL) 0.38 ± 0.23 Cmax (μg/mL) 0.06 ± 0.01 T1/2 (h) 10.62 ± 2.31
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| References |
[1]. Huang D, et al. Identification of a binding site on soluble RANKL that can be targeted to inhibit soluble RANK-RANKL interactions and treat osteoporosis. Nat Commun. 2022 Sep 12;13(1):5338.
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