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