MCF-7 (luminal), MDA-MB-231 (claudin-low), MDA-MB-468 (basal-like), and SkBr3 (HER2-OE) cells are all inhibited by pyrvinium pamoate (0-500 nM) in a dose-dependent manner. The MDA-MB-231 cell line's IC50 value is 1170±105.0 nM. Pividin pamoate produces BCSC populations with distinct characteristics by strongly inhibiting BCSC self-renewal and duplication. At the topological level, pividin pamoate dramatically decreased the average expression levels of FZD1, FZD10, WNT1, WNT7B, CTNNB1, MYC, and LRP5. Additionally, ALDH1, CD44, and ABCG2 expression are among the other stemness genes whose expression is successfully rearranged by pyrvinium pamoate[1]. Pyrvinium pamoate exhibits dose-dependent inhibition of the circular waveform (IC50), with a broad range of inhibitory concentrations (0.6 - 65 μM) observed for the WNT signal's circular waveform. While pyrvinium pamoate does not harm CK1, it eventually suppresses Wnt signaling by reducing the messenger RNA (mRNA) of known WNT target genes, such as c-MYC [3]. Cardiovascular heart-forming fibroblasts are susceptible to the amplitude toxicity of pamoic acid (IC50=9.5 nM). Piravinium pamoate's cytotoxic effects on cardiac fibroblasts in the presence of glutamine deficit and yogurt [4].

MCF-7 (luminal)、MDA-MB-231 (claudin-low)、MDA-MB-468 (basal-like) 和 SkBr3 (HER2-OE) 细胞均受到双羟萘酸吡维铵 (0-500 nM) 的抑制剂量依赖性方式。 MDA-MB-231细胞系的IC50值为1170±105.0 nM。 Pividin 双羟萘酸盐通过强烈抑制 BCSC 自我更新和复制来产生具有独特特征的 BCSC 群体。在拓扑水平上，pividin 双羟萘酸盐显着降低了 FZD1、FZD10、WNT1、WNT7B、CTNNB1、MYC 和 LRP5 的平均表达水平。此外，ALDH1、CD44 和 ABCG2 表达属于其他干性基因，其表达可被双羟萘酸吡维尼盐成功重排[1]。 Pyrvinium pamoate 对圆形波形表现出剂量依赖性抑制 (IC50)，对 WNT 信号的圆形波形观察到的抑制浓度范围较广 (0.6 - 65 μM)。虽然吡维双羟萘酸盐不会损害 CK1，但它最终会通过减少已知 WNT 靶基因（例如 c-MYC）的信使 RNA (mRNA) 来抑制 Wnt 信号传导 [3]。心血管心脏形成成纤维细胞对双羟萘酸的毒性幅度敏感（IC50=9.5 nM）。在谷氨酰胺缺乏和酸奶存在的情况下，双羟萘酸吡维铵对心脏成纤维细胞具有细胞毒性作用[4]。

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双羟萘酸吡维铵 (PP) 在缺血条件下（3% 氧气，300 µM 葡萄糖，<100 µM 谷氨酰胺）培养的心脏成纤维细胞中表现出特异性细胞毒性作用，处理72小时后的IC50为9.5 nM。在正常培养条件下（20-21% 氧气，25 mM 葡萄糖，4 mM 谷氨酰胺），PP显示出最小的毒性。[4]
在缺血条件下，补充正常水平的氧气（20-21%）和谷氨酰胺（4 mM）不能挽救PP（87 nM）对心脏成纤维细胞的细胞毒性作用。[4]
在缺血条件下，补充正常水平的氧气（20-21%）和葡萄糖（25 mM）可以部分挽救PP（87 nM）的细胞毒性作用。[4]
在缺血条件下，补充正常水平的葡萄糖（25 mM）和谷氨酰胺（4 mM）可以完全挽救PP（87 nM）的细胞毒性作用。这表明PP的细胞毒性特异性依赖于葡萄糖，并在较小程度上依赖于谷氨酰胺的缺乏。[4]

Pyrvinium pamoate (500 nM) 显着减少异种移植模型中的肿瘤体积、肿瘤大小和重量，并严重延迟肿瘤[1]。

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在小鼠心肌梗塞模型（永久性左冠状动脉结扎）中，每日口服PP（从结扎后第1天开始）与载体对照组相比，在结扎后第4天显著减少了梗死区的增殖细胞（Ki67阳性）数量。[4]
PP治疗在结扎后第7天显著减少了边缘区和梗死区中α-平滑肌肌动蛋白（αSMA）阳性的心脏肌成纤维细胞数量。[4]
PP治疗在结扎后第14天显著减少了左心室的纤维化面积（通过Masson三色染色评估）和羟脯氨酸含量（成熟胶原的定量指标），而未改变第4天时的初始梗死面积。[4]
PP治疗改善了左心室收缩功能，通过超声心动图测量显示，在结扎后第14天，与载体治疗的梗塞小鼠相比，射血分数显著增加。[4]
PP治疗在结扎后第14天增加了瘢痕心脏组织中的微血管密度（CD31阳性毛细血管）。[4]

For the myocardial infarction mouse model, pyrvinium pamoate (PP) was suspended at a final concentration of 400 µg/ml in a vehicle consisting of 4% dimethyl sulfoxide (DMSO) in saline. Mice were force-fed (intragastrically) with 0.5 ml of this suspension daily. Oral administration began at 1 day after coronary artery ligation (post-ligation) and continued daily until the endpoint at 14 days post-ligation. The control group received the vehicle (4% DMSO in saline) following the same schedule. [4]

A previous study cited within the literature indicates that oral administration of PP at the same dosage used in this study resulted in clearance of the drug from the circulation within 12 hours. No further pharmacokinetic parameters (e.g., absorption, distribution, metabolism, excretion, half-life, bioavailability) are provided in this study. [4]

[1]. WNT pathway inhibitor pyrvinium pamoate inhibits the self-renewal and metastasis of breast cancer stem cells. Int J Oncol. 2016 Mar;48(3):1175-86.

[2]. The impact of pyrvinium pamoate on colon cancer cell viability. Int J Colorectal Dis. 2014 Oct;29(10):1189-98.

[3]. Pyrvinium pamoate does not activate protein kinase CK1, but promotes Akt/PKB down-regulation and GSK3 activation. Biochem J. 2013 May 15;452(1):131-7.

[4]. An anthelmintic drug, pyrvinium pamoate, thwarts fibrosis and ameliorates myocardial contractile dysfunction in a mouse model of myocardial infarction. PLoS One. 2013 Nov 4;8(11):e79374.

Pyrvinium pamoate appears as odorless bright orange or orange-red to brownish red or almost black fluffy powder. Melting point 210-215 °C. Insoluble in water. Tasteless.
Pyrvinium pamoate is a naphthoic acid. It has a role as an anticoronaviral agent.
Pyrvinium Pamoate is the pamoate salt of pyrvinium, a quinoline-derived cyanine dye and an mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with anthelmintic and potential antineoplastic activities. Upon administration, pyrvinium pamoate may inhibit mitochondrial OxPhos and mitochondrial respiration, decreases mitochondrial function, prevents tumor cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell proliferation and leading to tumor cell death in some types of cancer cells. Mitochondrial OxPhos is overactivated in cancer cells and plays a key role in tumor cell proliferation. Drug resistant tumor cells are very susceptible to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease in mitochondrial function by increasing glycolysis.
See also: Pyrvinium (has active moiety).

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Pyrvinium pamoate is an FDA-approved anthelmintic drug. [4]
The proposed mechanism in this study involves compromising the survival of cardiac fibroblasts specifically under conditions of glucose (and glutamine) deficiency, which mimics the ischemic microenvironment following myocardial infarction. This effect is similar to its previously reported activity against glucose-starved cancer cells. [4]
The study suggests a novel therapeutic application of PP for reducing fibrosis and improving function in scarred hearts after myocardial infarction, and potentially in other fibrotic organs/tissues. [4]
The timing of drug administration is critical. In this study, beneficial effects were observed when PP administration started one day after coronary ligation (after most cardiomyocyte death had occurred), rather than at the time of ligation. [4]

C75H70N6O6

1151.39

1150.535

3546-41-6

110-85-0 (cation);142-88-1 (adipate);3546-41-6 (pamoate); 548-84-5 (Cl); 35648-29-4 (Iodide);

54680693

Red to reddish brown solid powder

1.0104 (rough estimate)

829.27°C (rough estimate)

210-215° (softens at 190°)

1.6400 (estimate)

12.338

144.82

2

8

12

87

1120

0

CC1=CC(=C(N1C2=CC=CC=C2)C)/C=C/C3=[N+](C4=C(C=C(C=C4)N(C)C)C=C3)C.CC1=CC(=C(N1C2=CC=CC=C2)C)/C=C/C3=[N+](C4=C(C=C(C=C4)N(C)C)C=C3)C.C1=CC=C2C(=C(C(=CC2=C1)C(=O)O)[O-])CC3=C(C(=CC4=CC=CC=C34)C(=O)O)[O-]

OOPDAHSJBRZRPH-UHFFFAOYSA-L

InChI=1S/2C26H28N3.C23H16O6/c2*1-19-17-21(20(2)29(19)24-9-7-6-8-10-24)11-13-23-14-12-22-18-25(27(3)4)15-16-26(22)28(23)5;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h2*6-18H,1-5H3;1-10,24-25H,11H2,(H,26,27)(H,28,29)/q2*+1;/p-2

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。  (2). 该产品在溶液状态不稳定，请现配现用。

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

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；
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