BPC 157

Anti-ulcer peptidergic agent

新型胃肽BPC157对胃肠道和培养的肠神经元和胶质细胞具有细胞保护作用[3]。

BPC 157（10 μg/kg，10 ng/kg）每天腹腔注射一次（手术后第一次应用，处死前 24 小时最后一次应用）或溶解在饮用水中（0.16 μg/mL/12 ml/天，直至牺牲）在多发性硬化症毒性大鼠模型中。控制通常不治疗结肠吻合术或半胱胺结肠炎。两者同时被 BPC 157 有效治愈 [2]。

身体保护化合物（BPC）157是一种稳定的胃五肽。Predrag Sikiric的团队对其在不同器官和组织中的细胞保护作用进行了许多研究。他们的证据表明，BPC157在神经损伤和胃肠道溃疡中具有强大的细胞保护作用。然而，BPC157在胃肠道中的作用尚不清楚。众所周知，肠道产生人体内95%的5-羟色胺（5-HT）。肠粘膜中的5-HT刺激免疫细胞产生促炎介质。肠道5-羟色胺可能是肠道炎症生理作用和发病机制的关键因素。先前的证据表明，肠道5-羟色胺在炎症性肠病中起着重要作用。这些报告暗示，BPC157显著调节了大鼠大脑不同区域5-羟色胺的区域合成。到目前为止，BPC157的详细作用机制在胃肠道生理学和病理生理学中仍然难以捉摸。因此，本研究旨在通过研究肠5-HT的释放、培养的肠神经元的存活率、培养的肠道神经胶质细胞（EGCs）的增殖以及有和没有BPC157的肠道运动，阐明BPC157在胃肠道中的细胞保护机制[3]。

Stable gastric pentadecapeptide BPC 157 was suggested to link inflammatory bowel disease and multiple sclerosis, and thereby, shown to equally counteract the models of both of those diseases. For colitis, cysteamine (400 mg/kg intrarectally (1 ml/rat)) and colon-colon anastomosis (sacrifice at day 3, 5, 7, and 14) were used. BPC 157 (10 μg/kg, 10 ng/kg) was applied either intraperitoneally once time daily (first application immediately after surgery, last at 24 hours before sacrifice) or per-orally in drinking water (0.16 μg/ml/12 ml/day till the sacrifice) while controls simultaneously received an equivolume of saline (5 ml/kg) intraperitoneally or drinking water only (12 ml/day). A multiple sclerosis suited toxic rat model, cuprizone (compared with standard, a several times higher regimen, 2.5% of diet regimen + 1 g/kg intragastrically/day) was combined with BPC 157 (in drinking water 0.16 μg or 0.16 ng/ml/12 ml/day/rat + 10 μg or 10 ng/kg intragastrically/day) till the sacrifice at day 4. In general, the controls could not heal cysteamine colitis and colon-colon anastomosis. BPC 157 induced an efficient healing of both at the same time. Likewise, cuprizone-controls clearly exhibited an exaggerated and accelerated damaging process; nerve damage appeared in various brain areas, with most prominent damage in corpus callosum, laterodorsal thalamus, nucleus reunions, anterior horn motor neurons. BPC 157-cuprizone rats had consistently less nerve damage in all damaged areas, especially in those areas that otherwise were most affected. Consistently, BPC 157 counteracted cerebellar ataxia and impaired forelimb function. Thereby, this experimental evidence advocates BPC 157 in both inflammatory bowel disease and multiple sclerosis therapy[2].

[1]. Sikiric P, et al. Stable gastric pentadecapeptide BPC 157: novel therapy in gastrointestinal tract. Curr Pharm Des. 2011;17(16):1612-1632.
[2]. Klicek R, et al. Stable gastric pentadecapeptide BPC 157 heals cysteamine-colitis and colon-colon-anastomosis and counteracts cuprizone brain injuries and motor disability. J Physiol Pharmacol. 2013;64(5):597-612.
> [3]. Cytoprotective Mechanism of the Novel Gastric Peptide BPC157 in Gastrointestinal Tract and Cultured Enteric Neurons and Glial Cells. Neurosci Bull. 2019 Feb; 35(1): 167–170.

Bepecin is under investigation in clinical trial NCT02637284 (PCO-02 - Safety and Pharmacokinetics Trial).

C62H98N16O22

1419.53552

1418.704

C, 52.46; H, 6.96; N, 15.79; O, 24.79

137525-51-0

216441-24-6 (sodium);137525-51-0;1628202-16-3 (TFA);

9941957

GEPPPGKPADDAGLV

Typically exists as white to off-white solids at room temperature

1.4±0.1 g/cm3

1802.9±65.0 °C at 760 mmHg

1044.2±34.3 °C

0.0±0.6 mmHg at 25°C

1.576

-2.41

574Ų

16

24

39

100

3040

12

NCCCCC(C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(=O)O)C(C)C)=O)CC(C)C)=O)=O)C)=O)CC(=O)O)=O)CC(=O)O)=O)C)=O)=O)NC(CNC([C@@H]1CCCN1C([C@@H]1CCCN1C([C@@H]1CCCN1C([C@@H](NC(CN)=O)CCC(=O)O)=O)=O)=O)=O)=O

HEEWEZGQMLZMFE-RKGINYAYSA-N

InChI=1S/C62H98N16O22/c1-31(2)25-37(55(92)74-50(32(3)4)62(99)100)71-46(81)29-65-51(88)33(5)67-53(90)38(26-48(84)85)73-54(91)39(27-49(86)87)72-52(89)34(6)68-57(94)41-15-10-21-75(41)58(95)35(13-7-8-20-63)70-45(80)30-66-56(93)40-14-9-22-76(40)60(97)43-17-12-24-78(43)61(98)42-16-11-23-77(42)59(96)36(18-19-47(82)83)69-44(79)28-64/h31-43,50H,7-30,63-64H2,1-6H3,(H,65,88)(H,66,93)(H,67,90)(H,68,94)(H,69,79)(H,70,80)(H,71,81)(H,72,89)(H,73,91)(H,74,92)(H,82,83)(H,84,85)(H,86,87)(H,99,100)/t33-,34-,35-,36-,37-,38-,39-,40-,41-,42-,43-,50-/m0/s1

L-Valine, glycyl-L-alpha-glutamyl-L-prolyl-L-prolyl-L-prolylglycyl-L-lysyl-L-prolyl-L-alanyl-L-alpha-aspartyl-L-alpha-aspartyl-L-alanylglycyl-L-leucyl-

BPC 157; BPC-157; BPC157; Bpc 15; Bpc-15; Bpc15; Bpc 157; Bepecin; Bpc 15; Bpc157; Booly protection compound 15; L-Valine, glycyl-L-alpha-glutamyl-L-prolyl-L-prolyl-L-prolylglycyl-L-lysyl-L-prolyl-L-alanyl-L-alpha-aspartyl-L-alpha-aspartyl-L-alanylglycyl-L-leucyl-; Booly protection compound 15

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 : ≥ 100 mg/mL (~70.45 mM)
DMSO : ~50 mg/mL (~35.22 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (1.76 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: 2.5 mg/mL (1.76 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (1.76 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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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。