sRANKL-IN-3|cas:2412947-15-8|西域试剂

sRANKL-IN-3,98.95%

产品编号：Bellancom-151347| CAS NO：2412947-15-8| 分子式：C₁₆H₁₄N₄O₄| 分子量：326.31

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-151347	￥2000.00	杭州北京（现货）
Bellancom-151347	￥3500.00	杭州北京（现货）
Bellancom-151347	￥6500.00	杭州北京（现货）
Bellancom-151347	￥9500.00	杭州北京（现货）
Bellancom-151347	￥13500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

sRANKL-IN-3

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 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.

体外研究

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).
sRANKL-IN-3 (0.01-100 μM; 5 d; osteoclast) inhibits osteoclastogenesis in a dose-dependent manner.
sRANKL-IN-3 (5 μM; 24 h; osteoclast) suppresses RANKL mediated NF-κB and MAPK signaling pathway.
sRANKL-IN-3 (0.003-33 μM; 24 h; osteoclast) induces mature osteoclasts apoptosis and attenuates bone resorption in a dose-dependent manner.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female SD ovariectomy (OVX) rats
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

Dosage:

10 mg/kg

Administration:

Oral gavage (Pharmacokinetic Study)

Result:

The pharmacokinetic parameters of sRANKL-IN-3

	sRANKL-IN-2
AUC (hr*μg/mL)	113.59
C_max (μg/mL)	9.52
T_1/2 (h)	15.55

体内研究

sRANKL-IN-3 (Compound S3-15, 10 mg/kg/d; i.g.; 12 weeks) shows anti-osteoporosis activity in ovariectomy rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female SD ovariectomy (OVX) rats
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

Dosage:

10 mg/kg

Administration:

Oral gavage (Pharmacokinetic Study)

Result:

The pharmacokinetic parameters of sRANKL-IN-3

	sRANKL-IN-2
AUC (hr*μg/mL)	113.59
C_max (μg/mL)	9.52
T_1/2 (h)	15.55

体内研究

sRANKL-IN-3 (Compound S3-15, 10 mg/kg/d; i.g.; 12 weeks) shows anti-osteoporosis activity in ovariectomy rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female SD ovariectomy (OVX) rats
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

Dosage:

10 mg/kg

Administration:

Oral gavage (Pharmacokinetic Study)

Result:

The pharmacokinetic parameters of sRANKL-IN-3

	sRANKL-IN-2
AUC (hr*μg/mL)	113.59
C_max (μg/mL)	9.52
T_1/2 (h)	15.55

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (76.61 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

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)

参考文献