الصفحة الرئيسية>>Signaling Pathways>> Microbiology & Virology>> Parasite>>SID 26681509 quarterhydrate

SID 26681509 quarterhydrate

رقم الكتالوجGC61791

إن ربع هيدرات SID 26681509 هو مثبط قوي ، وقابل للعكس ، وتنافسي ، وانتقائي للكاثيبسين L البشري مع IC50 من 56 نانومتر

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SID 26681509 quarterhydrate التركيب الكيميائي

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
660٫00
متوفر
1 mg
181٫00
متوفر
5 mg
538٫00
متوفر
10 mg
908٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of SID 26681509 quarterhydrate

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[1].

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 (Ki = 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].

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

[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. [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.

Chemical Properties of SID 26681509 quarterhydrate

Cas No. SDF
Canonical 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
Formula C27H33N5O5S.1/4H2O M.Wt 544.16
الذوبان DMSO: 27 mg/mL (49.62 mM); Ethanol: 5 mg/mL (9.19 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SID 26681509 quarterhydrate

Prepare stock solution
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
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In vivo Formulation Calculator (Clear solution) of SID 26681509 quarterhydrate

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for SID 26681509 quarterhydrate

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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