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CA-074 Me
Cathepsin B抑制剂,CA-074 methyl ester 是一种特异性的 Cathepsin B 抑制剂,具有保护神经,抗癌、抗炎等多种生物活性。
目录号: PC15715 纯度: ≥98%
CAS No. :147859-80-1
商品编号 规格 价格 会员价 是否有货 数量
PC15715-1mg 1mg ¥686.00 请登录
PC15715-5mg 5mg ¥1176.00 请登录
PC15715-10mg 10mg ¥2058.00 请登录
PC15715-25mg 25mg ¥3822.00 请登录
PC15715-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥1029.00 请登录
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中文名称
CA-074 Me
中文别名
1-甲基-1H-咪唑-2-胺盐酸盐;L-trans-环氧琥珀酸- Ile-Pro-OMe丙醛;L-反式-环氧丁二酰基-Ile-Pro-OMe 丙胺;(L-3-反式-(丙基氨基甲酰)环氧乙烷-2-甲酰基)-L-异亮氨酰-L-脯氨酸甲酯;CA-074 甲酯;L-trans-环氧琥珀酸-Ile-Pro-OMe丙醛
英文名称
CA-074 Me
英文别名
L-Proline,N-[[(2S,3S)-3-[(propylamino)carbonyl]-2-oxiranyl]carbonyl]-L-isoleucyl-, methylester;(S)-Methyl 1-((2S,3S)-3-methyl-2-((2S,3S)-3-(propylcarbamoyl)oxirane-2-carboxamido)pentanoyl)pyrrolidine-2-carboxylate;CA-074 ME;L-TRANS-EPOXYSUCCINYL-ILE-PRO-OME PROPYLAMIDE;(L-3-trans-(Propylcarbamyl)oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester;CA074 methyl ester;CA-074 methyl ester;CA074Me;CATHEPSIN B INHIBITOR IV;L-trans-Epoxysuccinic Ile-Pro-OMe Propylamide;L-trans-Epoxysuccinyl-isoleucyl-proline methyl ester propylamide;CA-074(OME);L-trans-Epoxysuccinyl(propylamide)-Ile-P;(L-3-Trans-(propylcarbamoyl)oxirane-2-carbony;L-TRANS-EPOXYSUCCINYL (PROPYLAMIDE)-ILE-PRO-OME;N-((L-3-TRANS-(PROPYLAMINO)CARBONYL)-OXIRANE-2-CARBONYL)-ILE-PRO-OME;L-trans-Epoxysuccinic Ile-Pro-OMe Propylamide;CA 074Me;Methyl (2S)-1-[(2S,3S)-3-methyl-2-[[(2S,3R)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]py
Cas No.
147859-80-1
分子式
C19H31N3O6
分子量
397.47
包装储存
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

性状

Solid

体外研究(In Vitro)

CA-074Me (5 μM and 50 μM) inhibits RANKL-induced osteoclastogenesis in BMM cells derived from C57BL/6J and NOD/ShiLtJ mice. CA-074Me exerts its anti-osteoclastogenic effect within 24 hours post-RANKL stimulation 体外研究. CA-074Me does not exert its anti-osteoclastogenic effect via the MAPK-ERK signaling cascade. CA-074Me inhibits c-FOS upregulation and subsequent NFATc1 autoamplification following RANKL stimulation.. CA-074Me reduces apoptosis induced by CVB1.

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

体内研究(In Vivo)

Hippocampal CA1 neuronal programmed necrosis induced by global cerebral I/R injury is prevented by CA074-me (1 μg, 10 μg) both pre-treatment and post-treatment. The rupture of lysosomal membrane and the leakage of cathepsin-B, and this is strongly inhibited by CA074-me pre-treatment. The overexpression and nuclear translocation of RIP3 and the reduction of NAD level after I/R injury are also inhibited, while the upregulation of Hsp70 is strengthened by CA074-me pre-treatment. CA-074Me (30 mg/kg) is capable of inhibiting osteoclastogenesis and bone degradation in vivo. In the CVB+CA-074Me (4 mg/kg/day i.m.) guinea pigs group, the scores of inflammation significantly decrease in comparison with the CVB+None group. In CVB+CA-074Me group, the number of CD8T cells decrease in comparison with the sham group.

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

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (251.59 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5159 mL 12.5796 mL 25.1591 mL
5 mM 0.5032 mL 2.5159 mL 5.0318 mL
10 mM 0.2516 mL 1.2580 mL 2.5159 mL
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产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.29 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.29 mM,饱和度未知) 的澄清溶液。

    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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.29 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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