SID 26681509

Name: SID 26681509
Brand: MedChemExpress
SKU: HY-103353
Rating: 5.0 (5 reviews)

Cat. No.: HY-103353 Purity: 98.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC₅₀ of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC₅₀s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

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

SID 26681509 Chemical Structure

CAS No. : 958772-66-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 214	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 214	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of SID 26681509:

SID 26681509 quarterhydrate Get quote

5 Publications Citing Use of MCE SID 26681509

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•Related Screening Libraries:

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View All Cathepsin Isoform Specific Products:

View All Isoforms

Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

View All Parasite Isoform Specific Products:

View All Isoforms

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

cathepsin L

Plasmodium

Leishmania

In Vitro

After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC₅₀ of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M^-1s^-1 and koff = 2.2 × 10^-5 s^-1 (K_i = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148^[1].
SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC₅₀ values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G^[1].
SID 26681509 inhibits cathepsin V activity with an IC₅₀ value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability^[2].

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

In Vivo

SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models^[2].

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

Molecular Weight

539.65

Formula

C₂₇H₃₃N₅O₅S

CAS No.

958772-66-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=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 : 50 mg/mL (92.65 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	1.8531 mL	9.2653 mL	18.5305 mL
5 mM	0.3706 mL	1.8531 mL	3.7061 mL
10 mM	0.1853 mL	0.9265 mL	1.8531 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 1.25 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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: 98.70%

Select Batch:

Data Sheet (288 KB) SDS (251 KB)

COA (250 KB) HNMR (572 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Shah PP, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol. 2008 Jul;74(1):34-41. [Content Brief]

[2]. Pribis JP, et al. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015 Dec;21(1):749-757. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8531 mL	9.2653 mL	18.5305 mL	46.3263 mL
	5 mM	0.3706 mL	1.8531 mL	3.7061 mL	9.2653 mL
	10 mM	0.1853 mL	0.9265 mL	1.8531 mL	4.6326 mL
	15 mM	0.1235 mL	0.6177 mL	1.2354 mL	3.0884 mL
	20 mM	0.0927 mL	0.4633 mL	0.9265 mL	2.3163 mL
	25 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8531 mL
	30 mM	0.0618 mL	0.3088 mL	0.6177 mL	1.5442 mL
	40 mM	0.0463 mL	0.2316 mL	0.4633 mL	1.1582 mL
	50 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9265 mL
	60 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7721 mL
	80 mM	0.0232 mL	0.1158 mL	0.2316 mL	0.5791 mL

SID 26681509 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:

SID 26681509958772-66-2SID26681509SID-26681509CathepsinParasiteThiocarbazateslow-bindingpropagationmalariaLeishmaniamajorreversiblePlasmodiumfalciparuInhibitorinhibitorinhibit

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SID 26681509

Customer Review

Other Forms of SID 26681509:

SID 26681509 Related Antibodies

5 Publications Citing Use of MCE SID 26681509

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Cathepsin Isoform Specific Products:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

SID 26681509 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SID 26681509 Related Classifications

Keywords:

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