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雷尼酸锶 /Strontium Ranelate {[allProObj[0].p_purity_real_show]}

货号:A162052 同义名: S12911;Distrontium renelate

Strontium ranelate stimulates the calcium sensing receptors (CaSR) and leads to the differentiation of pre-osteoblast to osteoblast which increases the bone formation.

Strontium Ranelate 化学结构 CAS号:135459-87-9
Strontium Ranelate 化学结构
CAS号:135459-87-9
Strontium Ranelate 3D分子结构
CAS号:135459-87-9
Strontium Ranelate 化学结构 CAS号:135459-87-9
Strontium Ranelate 3D分子结构 CAS号:135459-87-9
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Strontium Ranelate 纯度/质量文件 产品仅供科研

货号:A162052 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CaSR 其他靶点 纯度
NPS-2143 ++++

Ca(2+) receptor, IC50: 43 nM

98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ROS,ERK,p38 MAPK 99%+
Fasudil HCl PKA,Rho 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 98%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 98%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 98%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 98%
Cinepazide Maleate 98%
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A Akt,p38 MAPK 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Strontium Ranelate 生物活性

描述 Extracellular calcium-sensing receptor (CaSR) is a heptahelical transmembrane-spanning G protein-coupled receptor (GPCR) that plays an essential role in maintaining extracellular calcium ion concentrations. Strontium ranelate is an agonist of CaR with an IC50 of 0.5 mM. It was shown that strontium ranelate treatment from 0.1 to 1 mM (Sr2+) for 5 days induced proliferation in mouse calvaria cells, and the mRNA expression of osteoblastic markers was significantly elevated after 22 days of treatment. On the contrary, 8 days of strontium ranelate treatment significantly decreased osteoclast differentiation in a dose-dependent manner, starting at 0.1 mM (Sr2+). Also in osteoclasts, reduced resorption was observed 48 hours after the treatment of 0.1 mM to 24 mM strontium ranelate (Sr2+)[3]. A murine study showed that a dose of 1800 mg/kg/d of strontium ranelate significantly increased the trabecular bone volume by 59% in female mice and by 38% in male mice after 104 weeks of treatment[4]. In adult ovariectomized rats, daily treatment of 625 mg/kg/day strontium ranelate for 52 weeks prevented their bone loss and micro-architecture deterioration[5]. A phase 3 clinical trial in postmenopausal women showed that daily ingestion of 2 g strontium ranelate reduced the risk of new vertebral fractures by 49% in the first year and by 41% over three years[6].
作用机制 Strontium ranelate contains two atoms of stable strontium (Sr2+), which resembles Ca2+, acting as an agonist of calcium-sensing receptor[7].

Strontium Ranelate 动物研究

Dose Rat: 25 mg/kg, 50 mg/kg[3] (p.o.) Dog: 25 mg/kg - 75 mg/kg[4] (p.o.)
Administration p.o.

Strontium Ranelate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02637180 - Completed - Greece ... 展开 >> NATIONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS, MEDICAL SCHOOL, 2nd DEPARTMENT OF ORTHOPAEDIC SURGERY Athens, Attiki, Greece, 14233 Democritus University of Thrace, School of Medicine, Department of Orthopaedic Surgery Alexandroupolis, Evros, Greece, 68100 Orthopaedic Department, Faculty of Medicine, School of Health Sciences, University of Thessalia Larissa, Greece, 41110 Aristotle University of Thessaloniki, 3rd University Orthopaedic Department, Papageorgiou General Hospital Thessaloniki, Greece, 56403 收起 <<
NCT00409032 Osteoporosis Phase 2 Completed - Denmark ... 展开 >> PhaseOneTrials Hvidovre, Denmark, 2650 Odense University Hospital Odense, Denmark, 5000 United Kingdom Medinova Clinic Northwood, Middlesex, United Kingdom Synexus Wales Clinical Research Centre Cardiff, United Kingdom, CF14 5GJ Synexus Scotland Clinical Research Centre Glasgow, United Kingdom, G81 2DR Synexus Limited Reading Clinical Research Centre Reading, United Kingdom, RG2 7AG University of Sheffield Sheffield, United Kingdom, S5 7AU Synexus Crosby Clinical Research Centre Waterloo, United Kingdom, L22 0LG Synexus Wigan Clinical Research Centre Wigan, United Kingdom, WN1 1XX 收起 <<
NCT00239629 Postmenopausal Osteoporosis Phase 4 Completed - Czech Republic ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Prague, Czech Republic, 128 21 Germany For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Hamburg, Germany, 20354 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Heidelberg, Germany, 69120 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Magdeburg, Germany, D-39110 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Vogelsang, Germany, 39245 Greece For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Kifissia, Greece, 145 61 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Thessaloniki, Greece, 56429 Israel For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Haifa, Israel, 31096 Mexico For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Guadalajara, Mexico, 44670 Spain For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Barcelona, Spain, 08025 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Madrid, Spain, 28041 收起 <<

Strontium Ranelate 参考文献

[1]Guo X, Wei S, et al. Dose-dependent Effects of Strontium Ranelate on Ovariectomy Rat Bone Marrow Mesenchymal Stem Cells and Human Umbilical Vein Endothelial Cells. Int J Biol Sci. 2016 Nov 25;12(12):1511-1522.

[2]Fernandez JM, Molinuevo MS, et al. Strontium ranelate prevents the deleterious action of advanced glycation endproducts on osteoblastic cells via calcium channel activation. Eur J Pharmacol. 2013 Apr 15;706(1-3):41-7.

[3]Bonnelye E, Chabadel A, Saltel F, Jurdic P. Dual effect of strontium ranelate: stimulation of osteoblast differentiation and inhibition of osteoclast formation and resorption in vitro. Bone. 2008 Jan;42(1):129-38.

[4]Delannoy P, Bazot D, Marie PJ. Long-term treatment with strontium ranelate increases vertebral bone mass without deleterious effect in mice. Metabolism. 2002 Jul;51(7):906-11.

[5]Bain SD, Jerome C, Shen V, Dupin-Roger I, Ammann P. Strontium ranelate improves bone strength in ovariectomized rat by positively influencing bone resistance determinants. Osteoporos Int. 2009 Aug;20(8):1417-28.

[6]Meunier PJ, Roux C, Seeman E, Ortolani S, Badurski JE, Spector TD, Cannata J, Balogh A, Lemmel EM, Pors-Nielsen S, Rizzoli R, Genant HK, Reginster JY. The effects of strontium ranelate on the risk of vertebral fracture in women with postmenopausal osteoporosis. N Engl J Med. 2004 Jan 29;350(5):459-68.

[7]Marie PJ. Strontium ranelate in osteoporosis and beyond: identifying molecular targets in bone cell biology. Mol Interv. 2010 Oct;10(5):305-12.

Strontium Ranelate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL

Strontium Ranelate 技术信息

CAS号135459-87-9
分子式C12H6N2O8SSr2
分子量 513.49
别名 S12911;Distrontium renelate;Strontium Ranelate, trade mane: Protelos or Proto.;S12911-2
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

H2O: 2 mg/mL(3.89 mM),配合低频超声,并水浴加热至45℃助溶

0.1 M HCL: 15 mg/mL(29.21 mM),配合低频超声,并调节pH至3

动物实验配方
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