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CA 074

Name: CA 074
Brand: TargetMol
SKU: T21509
Price: 73 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21509Cas No. 134448-10-5

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.

CA 074

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Purity: 98.81%

Catalog No. T21509Cas No. 134448-10-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$73	-	In Stock
5 mg	$222	-	In Stock
10 mg	$347	-	In Stock
25 mg	$695	-	In Stock
50 mg	$965	-	In Stock
100 mg	$1,280	-	In Stock
1 mL x 10 mM (in DMSO)	$187	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.81%

Appearance:Solid

Color:White

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COA HPLC HNMR MS

Product Introduction

Bioactivity

Description	CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.
Targets&IC50	Cathepsin B:2-5 nM(Ki)
In vitro	CA-074, a synthetic analogue of E-64 developed through rational drug design, is an irreversible inhibitor of most lysosomal cysteine proteinases. It exploits the dipeptidylcarboxypeptidase activity of cathepsin B. With a Ki of 2 to 5 nM, CA-074 selectively inhibits cathepsin B within living cells, provided that experimental conditions allow significant fluid-phase endocytosis of the drug[2]. Notably, CA-074 demonstrates significantly greater inhibitory effects on purified rat cathepsin B (10000-30000 times) compared to cathepsin H and L, for which the initial Kis are about 40-200 μM[3].
In vivo	The intraperitoneal injection of compound CA-074 into rats effectively and selectively inhibits cathepsin B activity[1]. Following intravenous administration of CA-074 immediately after the ischemic insult, it preserves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 minutes of brain ischemia. The extent of inhibition is excellent in three of eight monkeys and good in five of eight monkeys[1].

Chemical Properties

Molecular Weight	383.44
Formula	C₁₈H₂₉N₃O₆
Cas No.	134448-10-5
Smiles	[H][C@](NC(=O)[C@H]1O[C@@H]1C(=O)NCCC)([C@@H](C)CC)C(=O)N1CCC[C@H]1C(O)=O
Relative Density.	1.267 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (260.8 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.43 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6080 mL	13.0398 mL	26.0797 mL	130.3985 mL
5 mM	0.5216 mL	2.6080 mL	5.2159 mL	26.0797 mL
10 mM	0.2608 mL	1.3040 mL	2.6080 mL	13.0398 mL
20 mM	0.1304 mL	0.6520 mL	1.3040 mL	6.5199 mL
50 mM	0.0522 mL	0.2608 mL	0.5216 mL	2.6080 mL
100 mM	0.0261 mL	0.1304 mL	0.2608 mL	1.3040 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc