Day: February 22, 2023

A Monoclonal Antibody-Based Enzyme-Linked Immunosorbent Assay for Determination of Homoharringtonine was written by Pongkitwitoon, Benyakan;Sakamoto, Seiichi;Nagamitsu, Rika;Putalun, Waraporn;Tanaka, Hiroyuki;Morimoto, Satoshi. And the article was included in Planta Medica in 2018.Recommanded Product: 17388-39-5 This article mentions the following:

Homoharringtonine (HHT), also known as omacetaxine, is a natural compound found in the genus Cephalotaxusand is a promising pharmaceutical drug used for the treatment of chronic or accelerated phase chronic myeloid leukemia. As a tool for the quant. determination of HHT, a specific monoclonal antibody against HHT (MAb 6A1) was generated by conjugates prepared via sodium periodate-mediated oxidation The developed indirect competitive ELISA (icELISA) using MAb 6A1 was found to be highly specific and sensitive with a limit of detection for HHT of 48.8 ng/mL. Validation assays to evaluate precision and accuracy of the method were conducted by the use of intra- and inter-assay anal., recovery test, and comparison anal. between the amounts of HHT determined by ELISA and high-performance liquid chromatog. These results revealed that the established icELISA using MAb 6A1 is specific, sensitive, and reliable enough to be applied to the qual. anal. for HHT. Furthermore, the results of this study support the usefulness of sodium periodate as a reagent for the conjugation between Cephalotaxusalkaloids and proteins for producing specific antibodies. In the experiment, the researchers used many compounds, for example, (4aR,5R,6S)-4a-Hydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-5-vinyl-4,4a,5,6-tetrahydropyrano[3,4-c]pyran-1(3H)-one (cas: 17388-39-5Recommanded Product: 17388-39-5).

(4aR,5R,6S)-4a-Hydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-5-vinyl-4,4a,5,6-tetrahydropyrano[3,4-c]pyran-1(3H)-one (cas: 17388-39-5) belongs to tetrahydropyran derivatives. Tetrahydropyran is an important raw material and intermediate used in Organic Synthesis, Pharmaceuticals, Agrochemicals and dyestuff. The most notable anticancer agent, bryostatin, and eribulin are marine macrolides having intriguing tetrahydropyran and furan motif. Recommanded Product: 17388-39-5

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Dipole moments and conformation of 3- and 4-bromo- and chloroheteracyclohexanes was written by Remane, H.;Borsdorf, R.;Scholz, M.;Doelle, Erna;Loock, Petra. And the article was included in Journal fuer Praktische Chemie (Leipzig) in 1980.Synthetic Route of C5H9BrO This article mentions the following:

Dipole moments of I (Z = O, S, MeN, CH₂; X = Br, Cl) were determined exptl. and calculated by the CNDO/2 and vector addition methods. The dipole moments were used to calculate conformational free energies. The results are discussed in relation to NMR data for I. In the experiment, the researchers used many compounds, for example, 3-Bromo-tetrahydropyran (cas: 13047-01-3Synthetic Route of C5H9BrO).

3-Bromo-tetrahydropyran (cas: 13047-01-3) belongs to tetrahydropyran derivatives. Tetrahydropyrans and furans principally constitute as a central motif in diverse medicinally privileged molecules. The bismuth chloride-assisted cross-cyclization between homoallylic alcohols and epoxides provided various benzyl tetrahydropyran derivatives. The reaction afforded good yields of desired products and occurred under mild conditions.Synthetic Route of C5H9BrO

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation was written by Shimokawa, Kenichiro;Shibata, Norihito;Sameshima, Tomoya;Miyamoto, Naoki;Ujikawa, Osamu;Nara, Hiroshi;Ohoka, Nobumichi;Hattori, Takayuki;Cho, Nobuo;Naito, Mikihiko. And the article was included in ACS Medicinal Chemistry Letters in 2017.COA of Formula: C14H23BN2O3 This article mentions the following:

Protein degradation technol. based on hybrid small mols. is an emerging drug modality that has significant potential in drug discovery and as a unique method of post-translational protein knockdown in the field of chem. biol. Here, we report the first example of a novel and potent protein degradation inducer that binds to an allosteric site of the oncogenic BCR-ABL protein. BCR-ABL allosteric ligands were incorporated into the SNIPER (Specific and Nongenetic inhibitor of apoptosis protein [IAP]-dependent Protein Erasers) platform, and a series of in vitro biol. assays of binding affinity, target protein modulation, signal transduction, and growth inhibition were carried out. One of the designed compounds, I (SNIPER(ABL)-062), showed desirable binding affinities against ABL1, cIAP1/2, and XIAP and consequently caused potent BCR-ABL degradation In the experiment, the researchers used many compounds, for example, 1-(Tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (cas: 903550-26-5COA of Formula: C14H23BN2O3).

1-(Tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (cas: 903550-26-5) belongs to tetrahydropyran derivatives. Dihydropyrans and tetrahydropyrans are examples of cyclic ethers widespread in nature. There is large number of marine macrolide natural products that contain tetrahydropyran and tetrahydrofuran ring together. For instance, goniodomin A (actin targeting polyether), prorocentrolide (toxin halistatins), and percentotoxineCOA of Formula: C14H23BN2O3

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Genome-Edited Coincidence and PMP22-HiBiT Fusion Reporter Cell Lines Enable an Artifact-Suppressive Quantitative High-Throughput Screening Strategy for PMP22 Gene-Dosage Disorder Drug Discovery was written by Martinez, Natalia J.;Braisted, John C.;Dranchak, Patricia K.;Moran, John J.;Larson, Hunter;Queme, Bryan;Pak, Evgenia;Dutra, Amalia;Rai, Ganesha;Cheng, Ken Chih-Chien;Svaren, John;Inglese, James. And the article was included in ACS Pharmacology & Translational Science in 2021.Product Details of 11024-24-1 This article mentions the following:

Charcot-Marie-Tooth 1A (CMT1A) is the most common form of hereditary peripheral neuropathies, characterized by genetic duplication of the critical myelin gene Peripheral Myelin Protein 22 (PMP22). PMP22 overexpression results in abnormal Schwann cell differentiation, leading to axonal loss and muscle wasting. Since regulation of PMP22 expression is a major target of therapeutic discovery for CMT1A, we sought to establish unbiased approaches that allow the identification of therapeutic agents for this disease. Using genome editing, we generated a coincidence reporter assay that accurately monitors Pmp22 transcript levels in the S16 rat Schwann cell line, while reducing reporter-based false positives. A quant. high-throughput screen (qHTS) of 42 577 compounds using this assay revealed diverse novel chem. classes that reduce endogenous Pmp22 transcript levels. Moreover, some of these classes show pharmacol. specificity in reducing Pmp22 over another major myelin-associated gene, Mpz (Myelin protein zero). Finally, to investigate whether compound-mediated reduction of Pmp22 transcripts translates to reduced PMP22 protein levels, we edited the S16 genome to generate a reporter assay that expresses a PMP22-HiBiT fusion protein using CRISPR/Cas9. Overall, we present a screening platform that combines genome edited cell lines encoding reporters that monitor transcriptional and post-translational regulation of PMP22 with titration-based screening (e.g., qHTS), which could be efficiently incorporated into drug discovery campaigns for CMT1A. In the experiment, the researchers used many compounds, for example, Digitonin (cas: 11024-24-1Product Details of 11024-24-1).

Digitonin (cas: 11024-24-1) belongs to tetrahydropyran derivatives. Tetrahydropyran is a useful synthetic intermediate. Tetrahydropyranyl (THP-) ethers derived from the reaction of alcohols and dihydropyran are common intermediates in organic synthesis. There is large number of marine macrolide natural products that contain tetrahydropyran and tetrahydrofuran ring together. For instance, goniodomin A (actin targeting polyether), prorocentrolide (toxin halistatins), and percentotoxineProduct Details of 11024-24-1

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Evaluation of the in vitro/in vivo drug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition was written by Zheng, Yu Fen;Bae, Soo Hyeon;Choi, Eu Jin;Park, Jung Bae;Kim, Sun Ok;Jang, Min Jung;Park, Gyu Hwan;Shin, Wan Gyoon;Oh, Euichaul;Bae, Soo Kyung. And the article was included in Food and Chemical Toxicology in 2014.HPLC of Formula: 112246-15-8 This article mentions the following:

We evaluated the potential of BST204, a purified dry extract of ginseng, to inhibit or induce human liver cytochrome P 450 enzymes (CYPs) and UDP-glucuronosyltransferases (UGTs) in vitro to assess its safety. In vitro drug interactions of four bioactive ginsenosides of BST204, S-Rg3, R-Rg3, S-Rh2, and R-Rh2, were also evaluated. We demonstrated that BST204 slightly inhibited CYP2C8, CYP2D6, CYP2C9, and CYP2B6 activities with IC₅₀ values of 17.4, 26.8, 31.5, and 49.7 渭g/mL, resp. BST204 also weakly inhibited UGT1A1, UGT1A9, and UGT2B7 activities with IC₅₀ values of 14.5, 26.6, and 31.5 渭g/mL, resp. The potential inhibition by BST204 of the three UGT activities might be attributable to S-Rg3, at least in part, as its inhibitory pattern was similar to that of BST204. However, BST204 showed no time-dependent inactivation of the nine CYPs studied. In addition, BST204 did not induce CYP1A2, 2B6, or 3A4/5. On the basis of an in vivo interaction studies, our data strongly suggest that BST204 is unlikely to cause clin. significant drug-drug interactions mediated via inhibition or induction of most CYPs or UGTs involved in drug metabolism in vivo. Our findings offer a clearer understanding and possibility to predict drug-drug interactions for the safe use of BST204 in clin. practice. In the experiment, the researchers used many compounds, for example, 20(R)-Ginsenoside Rh2 (cas: 112246-15-8HPLC of Formula: 112246-15-8).

20(R)-Ginsenoside Rh2 (cas: 112246-15-8) belongs to tetrahydropyran derivatives. Dihydropyrans and tetrahydropyrans are examples of cyclic ethers widespread in nature. The bismuth chloride-assisted cross-cyclization between homoallylic alcohols and epoxides provided various benzyl tetrahydropyran derivatives. The reaction afforded good yields of desired products and occurred under mild conditions.HPLC of Formula: 112246-15-8

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Inhibitory effect of ginsenosides from steamed ginseng-leaves and flowers on the LPS-stimulated IL-12 production in bone marrow-derived dendritic cells was written by Nguyen, Huu Tung;Quang, Tran Hong;Son, Jeong-Hyun;Koo, Jung-Eun;Hong, Hye-Jin;Koh, Young-Sang;Song, Gyu Yong;Kim, Young Ho. And the article was included in Archives of Pharmacal Research in 2011.Safety of 20(R)-Ginsenoside Rh2 This article mentions the following:

Interleukin-12, a heterodimeric cytokine comprising p40 and p35 subunits, plays an essential role in the regulating the differentiation of Th cells, which establish and maximize the capabilities of the immune system. The aim of present study is to screen the effect of 21 ginsenosides from steamed ginseng-leaves and flowers on IL-12 production in bone marrow-derived dendritic cells induced by lipopolysaccharide. Noticeably, ginsenoside Rg₆ and ginsenoside F₄ exhibited particularly inhibitory effect on LPS-induced IL-12 production with the inhibition values of 80 and 82%; and ginsenoside ST₁ , ginsenoside SL₂ , ginsenoside SL₃ , ginsenoside Rh₃, ginsenoside Rk₂, and ginsenoside Rs₄ showed moderate effects with inhibition rates of 63, 65, 67, 68, 71, 73, and 67%, resp. These results warrant further studies concerning potential of saponin extracts of steamed ginseng-leaves and flowers for medicinal uses. In the experiment, the researchers used many compounds, for example, 20(R)-Ginsenoside Rh2 (cas: 112246-15-8Safety of 20(R)-Ginsenoside Rh2).

20(R)-Ginsenoside Rh2 (cas: 112246-15-8) belongs to tetrahydropyran derivatives. Numerous natural products have tetrahydropyran skeleton as the building block for designing new natural products and their derivatives e.g. aplysiatoxins, avermectins, oscillatoxins, talaromycins, latrunculins and acutiphycins. There is large number of marine macrolide natural products that contain tetrahydropyran and tetrahydrofuran ring together. For instance, goniodomin A (actin targeting polyether), prorocentrolide (toxin halistatins), and percentotoxineSafety of 20(R)-Ginsenoside Rh2

Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics