sRANKL-IN-3 (Compound S3-15) 是一种选择性的和具有口服活性的可溶性 RANKL (sRANKL) 抑制剂，其IC50为 0.19 μM。sRANKL-IN-3 可靶向抑制可溶性 RANK-RANKL 相互作用。sRANKL-IN-3 可用于骨质疏松症的研究。
| 生物活性 | sRANKL-IN-3 (Compound S3-15) is a potent, orally active and selectivesolubleRANKL(sRANKL)inhibitor with anIC50of 0.19 μM. sRANKL-IN-3 can be targeted to inhibit soluble RANK-RANKL interactions. sRANKL-IN-3 can be used for the research of osteoporosis[1]. |
体外研究
(In Vitro) | sRANKL-IN-3 (Compound S3-15) selectively binds sRANKL. sRANKL-IN-3 has a high binding affinity to sRANKL (KD=5.78 μM) and is significantly stronger than binary-RANKL (KD=124 μM)[1].
sRANKL-IN-3 (0.01-100 μM; 5 d; osteoclast) inhibits osteoclastogenesis in a dose-dependent manner[1].
sRANKL-IN-3 (5 μM; 24 h; osteoclast) suppresses RANKL mediated NF-κB and MAPK signaling pathway[1].
sRANKL-IN-3 (0.003-33 μM; 24 h; osteoclast) induces mature osteoclasts apoptosis and attenuates bone resorption in a dose-dependent manner[1].
sRANKL-IN-3 (0.1-10 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].
Cell Viability Assay[1] | Cell Line: | Osteoclast | | Concentration: | 0.01, 0.1, 1, 10, and 100 μM | | Incubation Time: | 5 days | | Result: | Inhibited osteoclastogenesis with an IC50value of 0.19 μM. |
Apoptosis Analysis[1] | Cell Line: | Mature osteoclasts | | Concentration: | 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3 10 and 33 μM | | Incubation Time: | 24 hours | | Result: | Significantly increased apoptosis of mature osteoclasts with an EC50of 0.55 μM. |
Apoptosis Analysis[1] | Cell Line: | C3H10T12 cells | | Concentration: | 0.1,1 and 10 μM | | Incubation Time: | 14 days | | Result: | Increased cell proliferation and mineralization in mouse embryonic mesenchymal stem cell line |
Western Blot Analysis[1] | Cell Line: | Osteoclast | | Concentration: | 5 μM | | Incubation Time: | 24 hours | | Result: | Reduced NF-κB and NFATC-luciferase expression and suppresses osteoclast markers (DC-stamp, Ctsk, MMP9, Tracp, Oscar, and Calcr) expression. |
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体内研究
(In Vivo) | sRANKL-IN-3 (Compound S3-15, 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-3[1]
| sRANKL-IN-2 | | AUC (hr*μg/mL) | 113.59 | | Cmax(μg/mL) | 9.52 | | T1/2(h) | 15.55 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(76.61 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.0646 mL | 15.3229 mL | 30.6457 mL | | 5 mM | 0.6129 mL | 3.0646 mL | 6.1291 mL | | 10 mM | 0.3065 mL | 1.5323 mL | 3.0646 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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