Calpeptin

Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

CAS No. 117591-20-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
200mg	JPY 112000	国内在庫あり
1g	JPY 298500	国内在庫なし(納期7~10日)

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文献中Selleckの製品使用例（22）

カスタマーフィードバック1个实验数据

質量管理及び製品安全説明書

現在のバッチを見る： 純度：>97%

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Calpeptin関連製品

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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	もっと見る

Cysteine Protease阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74 assessed as inhibition of PLC-epsilon overexpression-induced EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74/rheb assessed as reduction in EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-LC3 assessed as increase in EGFP-LC3 vesicle at 50 uM after 24 hrs	18391949
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced calpain activity by measuring Filamin-A levels at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced EMT by measuring alpha-SMA expression at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
HeLa	Autophagy assay	50 uM		Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 50 uM in presence of 400 nM bafilomycin A1	18391949
HeLa	Antiviral assay			Antiviral activity against human rhinovirus-14 in HeLa cells, IC50=17.7μM.	ChEMBL
HeLa	Cytotoxic assay			Cytotoxic activity against HeLa cells using XTT assay, TC50=22.1μM.	ChEMBL
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生物活性

製品説明

Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

Targets

Calpain II (porcine kidney) ^[1]	Calpain I (human platelets) ^[1]	Calpain I (porcine erythrocytes) ^[1]	Papainb ^[1]
34 nM(ID50)	40 nM(ID50)	52 nM(ID50)	138 nM(ID50)

In Vitro
In vitro	Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. ^[1] In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. ^[2] In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection. ^[3]
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Immunofluorescence	Src / EGFR		29641465

In Vivo
In Vivo	In a feline right ventricular (RV) PO (RVPO) model, calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death. ^[4] In a rat focal cerebral ischemia–reperfusion injury model, Calpeptin reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3. ^[5]
動物実験	動物モデル	Feline right ventricular (RV) PO (RVPO) model
	投与量	0.6 mg/kg
	投与経路	i.v.

参考
[1] Tsujinaka T, et al. Biochem Biophys Res Commun. 1988, 153(3), 1201-1208. [2] Pintér M, et al. Neurosci Lett. 1994, 170(1), 91-93 [3] Das A, et al. Brain Res. 2006, 1084(1), 146-157. [4] Mani SK, et al. Am J Physiol Heart Circ Physiol. 2008, 295(1), H314-326. [5] Peng S, et al. Mol Biol Rep. 2011, 38(2), 905-912. + 展開

参考

+ 展開

化学情報

分子量	362.46	化学式	C₂₀H₃₀N₂O₄
CAS No.	117591-20-5	SDF	Download Calpeptin SDFをダウンロードする
Smiles	CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 72 mg/mL ( (198.64 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 72 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):