CA-074 Me|147859-80-1|(CA-074Me)-陌孚医药/Medlife

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CA-074 Me (Synonyms: CA-074Me)

目录号: PC15715 纯度: ≥98%

CAS No. :147859-80-1

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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

[1]. Xu Y, et al. Protective mechanisms of CA074-me (other than cathepsin-B inhibition) against programmed necrosis induced by global cerebral ischemia/reperfusion injury in rats. Brain Res Bull. 2016 Jan;120:97-105 [Information]

[2]. Patel N, et al. CA-074Me compound inhibits osteoclastogenesis via suppression of the NFATc1 and c-FOS signaling pathways. J Orthop Res. 2015 Oct;33(10):1474-86 [Information]

[3]. Zhang L, et al. Treatment with CA-074Me, a Cathepsin B inhibitor, reduces lung interstitial inflammation and fibrosis in a rat model of polymyositis. Lab Invest. 2015 Jan;95(1):65-77 [Information]

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

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。

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产品使用指南

Data Sheet

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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