SID 26681509 quarterhydrate

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

製品番号: HY-103353A 純度: 98.02%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC₅₀ of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

SID 26681509 quarterhydrate 構造式

容量	価格（税別）	在庫状況	数量
1 mg	$195	在庫あり	Estimated Time of Arrival: December 31
5 mg	$580	在庫あり	Estimated Time of Arrival: December 31
10 mg		お問い合わせ
50 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of SID 26681509 quarterhydrate:

SID 26681509 在庫あり

顧客検証

Cathepsin アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

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

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

Plasmodium

体外実験

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.

体内実験

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.

分子量

544.16

分子式

C₂₇H₃₃N₅O₅S.1/4H₂O

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.[1/4].O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (91.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 5 mg/mL (9.19 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8377 mL	9.1885 mL	18.3769 mL
5 mM	0.3675 mL	1.8377 mL	3.6754 mL
10 mM	0.1838 mL	0.9188 mL	1.8377 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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 1.67 mg/mL (3.07 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.

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.

純度とドキュメンテーション

純度: 98.02%

Select Batch:

データシート (289 KB) SDS (251 KB)

COA (251 KB) LCMS (101 KB) Elemental Analysis Report (110 KB)

取扱説明書 (2659 KB)

参考文献

[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

Ethanol / DMSO	1 mM	1.8377 mL	9.1885 mL	18.3769 mL	45.9424 mL
Ethanol / DMSO	5 mM	0.3675 mL	1.8377 mL	3.6754 mL	9.1885 mL
DMSO	10 mM	0.1838 mL	0.9188 mL	1.8377 mL	4.5942 mL
	15 mM	0.1225 mL	0.6126 mL	1.2251 mL	3.0628 mL
	20 mM	0.0919 mL	0.4594 mL	0.9188 mL	2.2971 mL
	25 mM	0.0735 mL	0.3675 mL	0.7351 mL	1.8377 mL
	30 mM	0.0613 mL	0.3063 mL	0.6126 mL	1.5314 mL
	40 mM	0.0459 mL	0.2297 mL	0.4594 mL	1.1486 mL
	50 mM	0.0368 mL	0.1838 mL	0.3675 mL	0.9188 mL
	60 mM	0.0306 mL	0.1531 mL	0.3063 mL	0.7657 mL
	80 mM	0.0230 mL	0.1149 mL	0.2297 mL	0.5743 mL