2. Membrane Transporter/Ion Channel
  3. Sodium Phosphate Cotransporter
  4. EOS789

EOS789 是一种口服有效的钠依赖性磷酸转运蛋白抑制剂，其对人 NaPi-IIb、PiT-1、PiT-2 的 IC50 值分别为 6.8、1.5 和 1.7 μM；对大鼠 NaPi-IIb、PiT-1、PiT-2 的 IC50 分别为 3.9、1.9 和 1.7 μM。EOS789 可抑制肠道磷吸收，增加粪便磷排泄，减少尿磷排泄，降低血清磷酸盐、FGF23 和成体甲状旁腺激素水平。EOS789 可改善异位胸主动脉钙化、肾脏损伤和高磷血症，并抑制纤维化标志物的表达。EOS789 可用于研究高磷血症及慢性肾脏病-矿物质骨病 (CKD-MBD)。

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EOS789

EOS789 Chemical Structure

CAS No. : 1628848-73-6

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EOS789 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EOS789 is an orally active sodium-dependent phosphate transporter inhibitor, with IC50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2, respectively; and IC50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2, respectively. EOS789 inhibits intestinal phosphate absorption, increases fecal phosphate excretion, reduces urinary phosphate excretion, and decreases the levels of serum phosphate, FGF23, and adult parathyroid hormone. EOS789 ameliorates ectopic thoracic aortic calcification, renal injury and hyperphosphatemia, and inhibits the expression of fibrosis markers. EOS789 can be used for the research of hyperphosphatemia and chronic kidney disease-mineral and bone disorder (CKD-MBD)[1][2].

体外研究
(In Vitro)

EOS789 可抑制正常大鼠肠刷状缘膜囊泡的磷酸盐摄取，其 IC50 为 3.1 μM[1]。
EOS789 (0.3-3.0 μM; 24 h) 可剂量依赖性地抑制高磷酸盐诱导的人肾小球系膜细胞 hMes 130hT-9 中 Collagen 1A1、Collagen 3A1 及 α-平滑肌肌动蛋白 mRNA 的上调[2]。

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

EOS789 相关抗体:

Real Time qPCR[2]

Cell Line: hMes 130hT-9 immortalized human mesangial cells
Concentration: 0.3 μM, 1.0 μM, 3.0 μM
Incubation Time: 24 h
Result: Significantly suppressed Collagen 1A1 relative expression at 1.0 μM and 3.0 μM.
Significantly suppressed Collagen 3A1 relative expression at 1.0 μM and 3.0 μM.
Significantly suppressed α-smooth muscle actin relative expression at 3.0 μM.
Showed a dose-dependent inhibitory effect on all three fibrotic marker genes.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ F
Rat[1] 2 mg/kg i.v. 31900 ng·h/mL /
Rat[1] 20 mg/kg p.o. 22000 ng·h/mL 6.9 %
体内研究
(In Vivo)

EOS789 (0.050-0.50%；口服；每日一次；连续 3 天) 可剂量依赖性地增加正常雄性 Wistar 大鼠的粪便磷排泄量、减少尿磷排泄量并降低血清磷水平，证实其可抑制肠道磷吸收[1]。
EOS789 (0.015-1.0%；口服；每日一次；连续 14 天) 可剂量依赖性降低腺嘌呤诱导的高磷血症雄性 Wistar 大鼠的血清磷酸盐、FGF-23 和完整 PTH 水平，增加粪便磷排泄量并减少尿磷排泄量，且在等效剂量下其效力优于 NaPi-IIb 选择性抑制剂[1]。
EOS789 (0.3%；口服；自由摄取；第 21 天至第 116 天) 可持续性抑制慢性抗 Thy1.1 肾炎雄性 Fisher 大鼠的血清磷酸盐、FGF-23 及完整 PTH 水平，改善主动脉钙化，降低血清肌酐水平，并改善肾脏组织病理学及纤维化基因表达[1]。
EOS789 (0.3%；食物掺混；自由摄取；5 周) 可显著改善抗 GBM 诱导的肾小球肾炎大鼠的高磷血症、提升肾功能并减少肾小球新月体形成，同时可使血清肌酐显著降至 1.31 mg/dL，肾小球新月体形成占总肾小球的比例降至 66.1%[2]。

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

Animal Model: Crlj:WI (Wistar) (male)[1]
Dosage: 0.050%, 0.15%, 0.50%
Administration: p.o.; daily; 3 days
Result: Increased fecal 33P excretion rate from ~45% to ~55%.
Decreased urinary 33P excretion rate from ~4.5% to ~3%.
Decreased serum 33P radioactivity from ~3900 dpm/mL to ~3500 dpm/mL.
Increased fecal 33P excretion rate to ~60%.
Decreased urinary 33P excretion rate to ~2.2%.
Decreased serum 33P radioactivity to ~3200 dpm/mL.
Increased fecal 33P excretion rate to ~70%.
Decreased urinary 33P excretion rate to ~1.2%.
Decreased serum 33P radioactivity to ~2700 dpm/mL.
Animal Model: Crlj:WI (Wistar) (male, adenine-induced hyperphosphatemia)[1]
Dosage: 0.015%, 0.05%, 0.15%, 0.50%, 1.0%
Administration: p.o.; daily; 14 days
Result: Reduced serum phosphate from 9.7 mg/dl to ~7.5 mg/dl.
Reduced serum FGF-23 from ~10,000 pg/mL to ~1500 pg/mL.
Reduced serum intact PTH from ~700 pg/mL to ~450 pg/mL.
Reduced serum phosphate to ~6.8 mg/dl.
Reduced serum FGF-23 to ~1200 pg/mL.
Reduced serum intact PTH to ~350 pg/mL.
Reduced serum FGF-23 to ~800 pg/mL.
Reduced serum intact PTH to ~400 pg/mL.
Reduced serum FGF-23 to ~150 pg/mL.
Reduced serum intact PTH to ~100 pg/mL.
Reduced serum phosphate to ~6.5 mg/dl.
Increased fecal phosphorus excretion from ~78 mg/4d to ~120 mg/4d.
Decreased urinary phosphorus excretion from ~3.5 mg/d to near 0 mg/d.
Animal Model: F344/DuCrlCrlj (Fisher) (male, anti-Thy1.1-induced chronic kidney disease-mineral bone disorder)[1]
Dosage: 0.1%, 0.3%
Administration: p.o.; ad libitum; day 21 to day 116
Result: Reduced serum phosphate from ~12 mg/dl to ~10 mg/dl at study end.
Did not significantly reduce serum FGF-23 or intact PTH levels.
Showed no significant reduction in aortic calcium content.
Reduced serum phosphate to ~8 mg/dl.
Reduced serum FGF-23 from ~240,000 pg/mL to ~5000 pg/mL.
Reduced serum intact PTH from ~8000 pg/mL to ~4000 pg/mL.
Reduced serum creatinine from ~3.2 mg/dl to ~2.4 mg/dl.
Suppressed aortic calcium content to near normal levels, with no histopathologic calcification observed in any treated rats.
Reduced glomerulosclerosis score from 2.60 to 2.32, degeneration of tubules score from 2.54 to 2.23, and tubulointerstitial fibrosis score from 2.39 to 2.01.
Significantly reduced renal mRNA expression of TGF-β1, collagen type 1 α1, collagen type 3 α1, and α-smooth muscle actin versus disease control (0.3% dose).
Animal Model: Wistar (male, 7 weeks old, anti-rat GBM antibody-induced glomerulonephritis)[2]
Dosage: ~100 mg/kg/day; ~200 mg/kg/day
Administration: food admixture; ad libitum; 5 weeks
Result: Dose-dependently suppressed the disease-induced increase in serum phosphate.
Increased fecal phosphate excretion significantly to 89.1 mg/day.
Decreased fractional urinary phosphate excretion significantly to 18.5%.
Significantly suppressed serum FGF23 increase.
Significantly improved severely reduced serum calcitriol.
Decreased serum creatinine significantly to 1.31 mg/dL.
Decreased urinary fractional excretion of albumin significantly to 0.04%.
Decreased serum sodium significantly to 140.5 mEq/L.
Decreased urinary fractional excretion of sodium significantly to 1.15%.
Decreased glomerular crescent formation significantly to 66.1% of total glomeruli.
Significantly increased body weight compared to disease control.
Clinical Trial
分子量

772.70

Formula

C35H36F8N6O5
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (129.42 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2942 mL 6.4708 mL 12.9416 mL
5 mM 0.2588 mL 1.2942 mL 2.5883 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.24 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

EOS789 相关分类

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2942 mL 6.4708 mL 12.9416 mL 32.3541 mL
5 mM 0.2588 mL 1.2942 mL 2.5883 mL 6.4708 mL
10 mM 0.1294 mL 0.6471 mL 1.2942 mL 3.2354 mL
15 mM 0.0863 mL 0.4314 mL 0.8628 mL 2.1569 mL
20 mM 0.0647 mL 0.3235 mL 0.6471 mL 1.6177 mL
25 mM 0.0518 mL 0.2588 mL 0.5177 mL 1.2942 mL
30 mM 0.0431 mL 0.2157 mL 0.4314 mL 1.0785 mL
40 mM 0.0324 mL 0.1618 mL 0.3235 mL 0.8089 mL
50 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6471 mL
60 mM 0.0216 mL 0.1078 mL 0.2157 mL 0.5392 mL
80 mM 0.0162 mL 0.0809 mL 0.1618 mL 0.4044 mL
100 mM 0.0129 mL 0.0647 mL 0.1294 mL 0.3235 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EOS7891628848-73-6EOS 789EOS-789Sodium Phosphate CotransporterCHO-K1 cellsPiT-1chronic kidney disease-mineral and bone disorderNaPi-IIbNaPi-IIcNaPi-IIahMes 130hT-9 human mesangial cellsWistar ratsFisher ratsPiT-2Inhibitorinhibitorinhibit

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