Zoledronic acid monohydrate | 唑来膦酸一水合物 | Zoledronate monohydrate | Anti-resorptive Agant

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唑来磷酸一水化合物 /Zoledronic acid monohydrate {[allProObj[0].p_purity_real_show]}

货号：A211103 同义名： 唑来膦酸一水合物 / Zoledronate monohydrate;CGP42446A monohydrate

Zoledronic acid is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines.

Zoledronic acid monohydrate 化学结构
CAS号：165800-06-6

Zoledronic acid monohydrate 3D分子结构
CAS号：165800-06-6

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Zoledronic acid monohydrate 纯度/质量文件产品仅供科研

货号：A211103 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

PKC 亚型比较
转化生长因子-β 亚型比较

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									PKA,EGFR	95%
Dequalinium Chloride											99%+
Quercetin	✔									Src,Sirtuin	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 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。

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		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。

Zoledronic acid monohydrate 生物活性

描述

Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP) with potent anti-resorptive activity. It inhibits the differentiation and apoptosis of osteoclasts and also exhibits anti-cancer effects ^[1].

体内研究

Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) enhances bone mineral density and content ^[5].

Zoledronic Acid monohydrate (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) disrupts both osteoclast and osteoblast function, impacting bone remodeling in vivo and influencing bone mechanical properties ^[5].

体外研究

Zoledronic Acid monohydrate (0.1-1 µM; 48 hours) upregulates receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells ^[2].

Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells ^[2].

Zoledronic Acid monohydrate enhances RANKL expression via the IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells ^[2].

Zoledronic Acid monohydrate regulates osteoclast differentiation and function by modulating NF-κB and JNK signaling pathways ^[3].

Zoledronic Acid monohydrate (10-100 µM; 1-7 days) markedly reduces MC3T3-E1 cell viability ^[4].

Zoledronic Acid monohydrate (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells ^[4].

Zoledronic Acid monohydrate (10-100 µM; 4 days) decreases cell viability by inducing apoptosis ^[4].

Zoledronic Acid monohydrate exhibits inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µM ^[4].

Zoledronic acid monohydrate 参考文献

[1]Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.

[2]Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.

[3]Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.

[4]XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.

[5]Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.

Zoledronic acid monohydrate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.45mL

0.69mL

0.34mL

17.23mL

3.45mL

1.72mL

34.47mL

6.89mL

3.45mL

Zoledronic acid monohydrate 技术信息

CAS号	165800-06-6
分子式	C₅H₁₂N₂O₈P₂
分子量	290.105

别名	唑来膦酸一水合物 ;Zoledronate monohydrate;CGP42446A monohydrate;Zoledronic Acid (hydrate);CGP-4244 monohydrate;ZOL 446 monohydrate;CGP 42446 monohydrate
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

H₂O: 14 mg/mL(48.26 mM)，配合低频超声，并调节pH至8

动物实验配方

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