CA-074

Name: CA-074
Brand: MedChemExpress
SKU: HY-103350
Rating: 5.0 (14 reviews)

Cat. No.: HY-103350 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

For research use only. We do not sell to patients.

CA-074 Chemical Structure

CAS No. : 134448-10-5

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 228	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 228	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 840	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

IC₅₀ & Target

Ki: 2 to 5 nM (Cathepsin B)^[1]

In Vitro

CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug^[2]. CA-074 inhibits cathepsin B with a K_i of 2 to 5 nM, whereas the initial K_is for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity^[1]. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

383.44

Formula

C₁₈H₂₉N₃O₆

CAS No.

134448-10-5

Appearance

Solid

Color

White to yellow

SMILES

O=C(N1[C@@H](CCC1)C(O)=O)[C@@]([C@@H](C)CC)([H])NC([C@@H]2[C@@H](C(NCCC)=O)O2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (326.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6080 mL	13.0399 mL	26.0797 mL
5 mM	0.5216 mL	2.6080 mL	5.2159 mL
10 mM	0.2608 mL	1.3040 mL	2.6080 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (247 KB) HNMR (276 KB) RP-HPLC (248 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Towatari T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5. [Content Brief]

[2]. Montaser M, et al. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8. [Content Brief]

[3]. Yamashima T, et al. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33. [Content Brief]

Animal Administration
^[1]

Rats: Compound CA-074 or CA-030 or E-64 is injected intraperitoneally as a solution in saline containing DMSO. A dose of 8 mg/100 g body weight is injected. The rats are killed by a blow to the head 6 h after the injection, and their liver is perfused with saline, removed, weighed and chilled on ice. Samples of 4 g of liver are minced and homogenized. The homogenate is centrifuged at 800 xg for 15 min and the supernatant is centrifuged at 12000 xg for 30 min. The precipitate is suspended in 2 mL of 0.05 M acetate buffer, pH 5,0, and freeze-thawed for measurements of cathepsin B, H and L activities^[1].

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

References

[1]. Towatari T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5. [Content Brief]

[2]. Montaser M, et al. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8. [Content Brief]

[3]. Yamashima T, et al. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6080 mL	13.0398 mL	26.0797 mL	65.1992 mL
	5 mM	0.5216 mL	2.6080 mL	5.2159 mL	13.0398 mL
	10 mM	0.2608 mL	1.3040 mL	2.6080 mL	6.5199 mL
	15 mM	0.1739 mL	0.8693 mL	1.7386 mL	4.3466 mL
	20 mM	0.1304 mL	0.6520 mL	1.3040 mL	3.2600 mL
	25 mM	0.1043 mL	0.5216 mL	1.0432 mL	2.6080 mL
	30 mM	0.0869 mL	0.4347 mL	0.8693 mL	2.1733 mL
	40 mM	0.0652 mL	0.3260 mL	0.6520 mL	1.6300 mL
	50 mM	0.0522 mL	0.2608 mL	0.5216 mL	1.3040 mL
	60 mM	0.0435 mL	0.2173 mL	0.4347 mL	1.0867 mL
	80 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8150 mL
	100 mM	0.0261 mL	0.1304 mL	0.2608 mL	0.6520 mL

CA-074 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CA-074134448-10-5CA074CA 074CathepsinInhibitorinhibitorinhibit

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CA-074

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CA-074 Related Antibodies

14 Publications Citing Use of MCE CA-074

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

CA-074 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

CA-074 Related Classifications

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