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sRANKL-IN-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
sRANKL-IN-3图片
CAS NO:2412947-15-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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.
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
分子量

326.31

性状

Solid

Formula

C16H14N4O4

CAS 号

2412947-15-8

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0646 mL15.3229 mL30.6457 mL
5 mM0.6129 mL3.0646 mL6.1291 mL
10 mM0.3065 mL1.5323 mL3.0646 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。