柠檬酸三钠表现出剂量依赖性抗增殖作用（0–12.5 mM；24 小时）[3]。在 G2/M 和 S 期，柠檬酸三钠（12.5 mM；72 小时）剂量依赖性地促进细胞凋亡和细胞周期停滞 [3]。 48后FAS、BAX、BID、AIF、EndoG、细胞色素c、PARP、GADD153、GRP78和caspase-3、-8、-9的表达上调，BCL-2和BCL-Xl的表达下调12.5 mM 柠檬酸三钠下的反应时间[3]。

在小鼠肝脏中，腹腔注射柠檬酸三钠（120、240 和 480 mg/kg）可以显着降低 GSH-Px 活性并提高 MDA（丙二醛）水平 [1]。暴露于腹腔内柠檬酸三钠（120、240 和 480 mg/kg）的小鼠肝细胞表现出 caspase-3 活性的剂量依赖性增加，从而导致细胞凋亡 [1]。腹腔注射柠檬酸三钠（120、240 和 480 mg/kg；每周一次，持续三周）的小鼠会出现肾毒性 [2]。

细胞活力测定[3]
细胞类型： HaCaT 细胞
测试浓度： 0、2.5、5、7.5、10、12.5 mM
孵育持续时间：24小时
实验结果：以剂量依赖性方式抑制细胞活力。

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细胞周期分析[3]
细胞类型： HaCaT 细胞
测试浓度： 12.5 mM
孵育时间：0、12、24、48、72小时
实验结果：一次剂量诱导细胞凋亡和细胞周期停滞在G2/M期和S期-依赖方式Expect。

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蛋白质印迹分析[3]
细胞类型： HaCaT 细胞
测试浓度： 12.5 mM
孵育时间：12、24、48小时
实验结果：FAS、BAX、BID、AIF、EndoG、细胞色素c、PARP、GADD153、 GRP78 和 caspase -3、-8、-9 以及 BCL-2 和 BCL-X1 减少。

Animal/Disease Models: 20 g male Kunming mice [2]
Doses: 120, 240, 480 mg/kg
Route of Administration: intraperitoneal (ip) injection; once a week for 3 weeks.
Experimental Results: The activities of T-SOD and GSH-Px in the treatment group diminished with the increase of citric acid dose, the activity of NOS demonstrated an increasing trend, and the contents of H2O2 and MDA gradually diminished.

Absorption, Distribution and Excretion
Tmax of 98-130min.
Largely eliminated through hepatic metabolism with very little cleared by the kidneys.
19-39L.
Total clearance of 313-1107mL/min.
IN THE BODY, SODIUM CITRATE IS OXIDIZED TO BICARBONATE & EXCRETED IN THE URINE...

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Metabolism / Metabolites
Citrate is metabolized to bicarbonate in the liver and plays a role as an intermediate in the citric acid cycle.
IN THE BODY, SODIUM CITRATE IS OXIDIZED TO BICARBONATE...

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Biological Half-Life
18-54 min

[1]. Study on injury effect of food additive citric acid on liver tissue in mice. Cytotechnology. 2014 Mar;66(2):275-82.

[2]. Chen X, Lv Q, Liu Y, Deng W. Effects of the food additive, citric acid, on kidney cells of mice. Biotech Histochem. 2015 Jan;90(1):38-44.

[3]. Citric acid induces cell-cycle arrest and apoptosis of human immortalized keratinocyte cell line (HaCaT) via caspase- and mitochondrial-dependent signaling pathways. Anticancer Res. 2013 Oct;33(10):4411-20.

Sodium citrate is the trisodium salt of citric acid. It has a role as a flavouring agent and an anticoagulant. It contains a citrate(3-).
Sodium citrate is the sodium salt of citric acid. It is white, crystalline powder or white, granular crystals, slightly deliquescent in moist air, freely soluble in water, practically insoluble in alcohol. Like citric acid, it has a sour taste. From the medical point of view, it is used as alkalinizing agent. It works by neutralizing excess acid in the blood and urine. It has been indicated for the treatment of metabolic acidosis.
Sodium Citrate is the sodium salt of citrate with alkalinizing activity. Upon absorption, sodium citrate dissociates into sodium cations and citrate anions; organic citrate ions are metabolized to bicarbonate ions, resulting in an increase in the plasma bicarbonate concentration, the buffering of excess hydrogen ion, the raising of blood pH, and potentially the reversal of acidosis. In addition, increases in free sodium load due to sodium citrate administration may increase intravascular blood volume, facilitating the excretion of bicarbonate compounds and an anti-urolithic effect.
Sodium salts of citric acid that are used as buffers and food preservatives. They are used medically as anticoagulants in stored blood, and for urine alkalization in the prevention of KIDNEY STONES.
See also: Anticoagulant sodium citrate solution (has subclass); sodium chloride; sodium citrate, unspecified form (component of) ... View More ...

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Drug Indication
Used as an anticoagulant during plasmophoresis as well as a neutralizing agent in the treatment of upset stomach and acidic urine.
FDA Label

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Mechanism of Action
Citrate chelates free calcium ions preventing them from forming a complex with tissue factor and coagulation factor VIIa to promote the activation of coagulation factor X. This inhibits the extrinsic initiation of the coagulation cascade. Citrate may also exert an anticoagulant effect via a so far unknown mechanism as restoration of calcium concentration does not fully reverse the effect of citrate. Citrate is a weak base and so reacts with hydrochloric acid in the stomach to raise the pH. It it further metabolized to bicarbonate which then acts as a systemic alkalizing agent, raising the pH of the blood and urine. It also acts as a diuretic and increases the urinary excretion of calcium.

C6H5NA3O7

258.0690

257.972

68-04-2

Citric acid;77-92-9

6224

White to off-white solid powder

1.008 g/mL at 20 °C

300°C

140.62

1

7

2

16

211

0

HRXKRNGNAMMEHJ-UHFFFAOYSA-K

InChI=1S/C6H8O7.3Na/c7-3(8)1-6(13,5(11)12)2-4(9)10;;;/h13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);;;/q;3*+1/p-3

trisodium;2-hydroxypropane-1,2,3-tricarboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~50 mg/mL (~193.75 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。