sRANKL-IN-3
目录号 : GC68454sRANKL-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。
Cas No.:2412947-15-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
sRANKL-IN-3 (Compound S3-15) is a potent, orally active and selective soluble RANKL (sRANKL) inhibitor with an IC50 of 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].
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 IC50 value 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 EC50 of 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. |
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]
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[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.
| Cas No. | 2412947-15-8 | SDF | Download SDF |
| 分子式 | C16H14N4O4 | 分子量 | 326.31 |
| 溶解度 | 储存条件 | 4°C, away from moisture and light | |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。