PD 151746

μ-Calpain (IC50 = 260 nM); m-calpain (IC50 = 5.33 μM)

体外活性：在 SY5Y 细胞中，PD151746 有效减弱麦芽毒素诱导的 SLLVY-AMC 水解。在 HMEC-1 细胞中，PD 151746 降低氧化低密度脂蛋白 (oxLDL) 诱导的细胞毒性。激酶测定：PD151746 是一种钙蛋白酶抑制剂，对 u-钙蛋白酶 (Ki = 0.26 ± 0.03 μM) 的选择性是 m-钙蛋白酶 (Ki = 5.33 ± 0.77 μM) 的 20 倍。细胞测定：在小脑颗粒细胞中，PD151746 通过抑制钙蛋白酶，将血清/钾 (S/K) 撤除诱导的细胞凋亡抑制 29%。此外，PD151746 还能抑制 MEF2 磷酸化和 cdk5/p25 形成的增加，并抑制 caspase-3 活性。在人肝癌G2细胞中，PD151746显着减少胰岛素刺激的糖原合成并增加蛋白酪氨酸磷酸酶-ε（PTPε）的量，这表明钙蛋白酶在调节胰岛素刺激的糖原合成中发挥重要作用。在表达人甲酰肽受体 (hFPR) 或 hFPR 样 1 (hFPRL1) 的 HEK-293 细胞中，PD151746 增加细胞质游离 Ca2+ ([Ca2+]I)。

PD151746 是一种钙蛋白酶抑制剂，对 u-钙蛋白酶 (Ki = 0.26 ± 0.03 μM) 的选择性是 m-钙蛋白酶 (Ki = 5.33 ± 0.77 μM) 的 20 倍。

PD151746 通过阻断钙蛋白酶，阻止血清/钾 (S/K) 戒断诱导的小脑颗粒细胞凋亡达 29%。此外，PD151746 降低了 caspase-3 活性、cdk5/p25 形成以及 MEF2 磷酸化的增加。 PD151746 显着降低人肝癌 G2 细胞中胰岛素刺激的糖原合成，同时增加蛋白酪氨酸磷酸酶-ε (PTPε)，表明钙蛋白酶是调节胰岛素刺激的糖原合成的关键参与者。 PD151746 升高表达人甲酰肽受体 (hFPR) 或 hFPR 样 1 (hFPRL1) 的 HEK-293 细胞中的细胞质游离 Ca2+ ([Ca2+]I)。

[1]. Proc Natl Acad Sci U S A . 1996 Jun 25;93(13):6687-92.

[2]. Biochem J . 2003 Sep 1;374(Pt 2):403-11.

C11H8FNO2S

237.25

237.03

C, 55.69; H, 3.40; F, 8.01; N, 5.90; O, 13.49; S, 13.51

179461-52-0

Solid powder

C1=CC2=C(C=C1F)C(=CN2)/C=C(/C(=O)O)\S

HWMQHECFXSVZGN-KMKOMSMNSA-N

InChI=1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-

(Z)-3-(5-fluoro-1H-indol-3-yl)-2-sulfanylprop-2-enoic acid

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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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。