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RS 09

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RS 09 is a TLR4 agonist.

Category
Peptide Inhibitors
Catalog number
BAT-010715
CAS number
1449566-36-2
Molecular Formula
C31H49N9O9
Molecular Weight
691.78
RS 09
IUPAC Name
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoic acid
Synonyms
Ala-Pro-Pro-His-Ala-Leu-Ser; RS09; RS-09; L-Serine, L-alanyl-L-prolyl-L-prolyl-L-histidyl-L-alanyl-L-leucyl-; L-Alanyl-L-prolyl-L-prolyl-L-histidyl-L-alanyl-L-leucyl-L-serine
Appearance
White lyophilised solid
Purity
≥95%
Density
1.346±0.06 g/cm3(Predicted)
Boiling Point
1191.2±65.0°C(Predicted)
Sequence
APPHALS
Storage
Store at -20°C
Solubility
Soluble to 2 mg/ml in water
InChI
InChI=1S/C31H49N9O9/c1-16(2)11-20(27(44)38-22(14-41)31(48)49)36-25(42)18(4)35-26(43)21(12-19-13-33-15-34-19)37-28(45)23-7-5-9-39(23)30(47)24-8-6-10-40(24)29(46)17(3)32/h13,15-18,20-24,41H,5-12,14,32H2,1-4H3,(H,33,34)(H,35,43)(H,36,42)(H,37,45)(H,38,44)(H,48,49)/t17-,18-,20-,21-,22-,23-,24-/m0/s1
InChI Key
SHYNPSTXGFDOBD-HRALPVODSA-N
Canonical SMILES
CC(C)CC(C(=O)NC(CO)C(=O)O)NC(=O)C(C)NC(=O)C(CC1=CN=CN1)NC(=O)C2CCCN2C(=O)C3CCCN3C(=O)C(C)N
1. Malignancy Upgrade Rates of Radial Sclerosing Lesions at Breast Cancer Screening
Grayson L Baird,Ana P Lourenco,Linda DeMello,Pamela Yan Radiol Imaging Cancer . 2021 Nov;3(6):e210036. doi: 10.1148/rycan.2021210036.
Purpose To determine the upgrade rate for biopsy-proven radial scars and radial sclerosing lesions (RS). Materials and Methods In this retrospective study, radiology and pathology databases from two tertiary breast centers were searched to identify patients with biopsy-confirmed RS between March 1, 2012, and December 31, 2017, during which all mammography was performed with digital breast tomosynthesis (DBT). Adjunct modalities such as MRI or US are performed at our centers to better characterize lesions identified at DBT. Patient demographics, imaging, needle and excisional biopsies, and follow-up data were collected at the patient level. Clopper-Pearson interval estimate for upgrade was calculated for 95% confidence using PropCIs package with R version 4.1.0 (R Foundation for Statistical Computing) (1). Results During the study period, a total of 155 885 DBT examinations were performed. From these examinations, 146 biopsy-proven RS were identified in 142 women (median age, 58 years; age range, 26-87 years). A total of 80.1% (117 of 146) of all RS did not have associated atypia or malignancy, and 19.9% (29 of 146) had associated atypia at initial biopsy. A total of 66.7% (78 of 117) of RS without atypia or malignancy were surgically excised, 25.6% (30 of 117) were followed (median, 3 years; range, 1-7 years) with benign findings on imaging, and 7.7% (nine of 117) were lost to follow-up. The rate of malignancy upgrade was 0.9% (one of 117 [95% CI: 0.02, 4.7]); one RS without concurrent atypia or malignancy demonstrated invasive carcinoma at surgical excision. Conclusion RS without atypia had a low upgrade rate.Keywords:Mammography, Breast © RSNA, 2021.
2. Resistant starch type 2 from lotus stem: Ultrasonic effect on physical and nutraceutical properties
Faiza Jhan,Mohd Arif Dar,Nairah Noor,J L H Jenno,Adil Gani Ultrason Sonochem . 2021 Aug;76:105655. doi: 10.1016/j.ultsonch.2021.105655.
Resistant starch type 2 (RS) was isolated from lotus stem using enzymatic digestion method. The isolated RS was subjected to ultrasonication (US) at different sonication power (100-400 W). The US treated and untreated RS samples were characterized using dynamic light scattering (DLS), scanning electron microscopy (SEM), light microscopy and Fourier transform infrared spectroscopy (FT-IR). DLS revealed that particle size of RS decreased from 12.80 µm to 413.19 nm and zeta potential increased from -12.34 mV to -26.09 mV with the increase in sonication power. SEM revealed smaller, disintegrated and irregular shaped RS particles after ultrasonication. FT-IR showed the decreased the band intensity at 995 cm-1and 1047 cm-1signifying that US treatment decreased the crystallinity of RS and increased its amorphous character. The bile acid binding, anti-oxidant and pancreatic lipase inhibition activity of samples also increased significantly (p < 0.05) with the increase in sonication power. Increase in US power however increased the values of hydrolysis from 23.11 ± 1.09 to 36.06 ± 0.13% and gylcemic index from 52.39 ± 0.38 to 59.50 ± 0.11. Overall, the non-thermal process of ultrasonic treatment can be used to change the structural, morphological and nutraceutical profile of lotus stem resistant starch which can have great food and pharamaceutical applications.
3. Magnesium in major depression
Mihai Nechifor Magnes Res . 2009 Sep;22(3):163S-166S.
There are contradictory data regarding the levels of magnesium in patients with major depression (MD) and how antidepressants influence their concentration. Our results show erythrocyte magnesium in patients with MD (44.39 +/- 2.7 mg/L vs. 59.1 +/- 3.2 mg/L in control group, p < 0.05) and only in patients with severe MD (Hamilton score > 23) was a moderate decrease in plasmatic magnesium observed (17.7 +/- 1.5 mg/L vs. 22.9 +/- 3.3 mg/L in control group). Therapy with antidepressants from different groups and with different mechanisms of action, such as amytriptiline (25 mg x 3/day per os, 4 weeks) and sertraline (50 mg x 3/day per os, 4 weeks) leads to a significant increase of magnesium concentration in erythrocytes (57.6 +/- 4.5 mg/L after amytriptiline, respectively 56.9 +/- 3.2 mg/L after sertraline, p < 0.05 vs. before therapy). At the same time, in patients with MD, plasmatic levels of zinc were significantly decreased before therapy and increased after treatment with amytriptiline and sertraline (0.68 +/- 0.09 mg/L before treatment vs. 0.9 +/- 0.07 after amytriptiline). There is a positive correlation between concentrations of magnesium in erythrocytes and the clinical evolution of patients with MD. We consider that increasing intracellular concentration is a component of the antidepressant mechanism of sertraline and amytriptiline and maybe of other antidepressants. Anhedonia and autolytic tendencies are important elements of MD symptomatology. We tested the influence of MgCl2 0.2 mM/kg/day on a reward system using conditioned place preference (Panlab) in rats. Our data show a moderate stimulation of the reward system by magnesium (290.6 +/- 27 s time spent in a conditioned compartment before magnesium treatment and 363.3 +/- 16 s after magnesium treatment) that reflects a stimulation of the reward system (RS). We consider that a magnesium-induced stimulation of the RS is an important issue for treating anhedonia in patients with MD. An increase of intracellular magnesium may be part of the mechanism of action of antidepressants.
4. Recommender Systems in Antiviral Drug Discovery
Maxim V Fedorov,Sergey Sosnin,Ivan Nazarov,Dmitry I Osolodkin,Anastasia A Nikitina,Ekaterina A Sosnina ACS Omega . 2020 Jun 21;5(25):15039-15051. doi: 10.1021/acsomega.0c00857.
Recommender systems (RSs), which underwent rapid development and had an enormous impact on e-commerce, have the potential to become useful tools for drug discovery. In this paper, we applied RS methods for the prediction of the antiviral activity class (active/inactive) for compounds extracted from ChEMBL. Two main RS approaches were applied: collaborative filtering (Surprise implementation) and content-based filtering (sparse-group inductive matrix completion (SGIMC) method). The effectiveness of RS approaches was investigated for prediction of antiviral activity classes ("interactions") for compounds and viruses, for which some of their interactions with other viruses or compounds are known, and for prediction of interaction profiles for new compounds. Both approaches achieved relatively good prediction quality for binary classification of individual interactions and compound profiles, as quantified by cross-validation and external validation receiver operating characteristic (ROC) score >0.9. Thus, even simple recommender systems may serve as an effective tool in antiviral drug discovery.
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