Category: Pyrazines

Feno, Simona; Di Marco, Giulia; De Mario, Agnese; Monticelli, Halenya; Reane, Denis Vecellio published an article in 2019, the title of the article was High-throughput screening using photoluminescence probe to measure intracellular calcium levels.Synthetic Route of 55779-48-1 And the article contains the following content:

Aequorin, a 22 kDa protein produced by the jellyfish Aequorea victoria, was the first probe used to measure Ca2+ concentrations ([Ca2+]) of specific intracellular organelles in intact cells. After the binding of Ca2+ to three high-affinity binding sites, an irreversible reaction occurs leading to the emission of photons that is proportional to [Ca2+]. While native aequorin is suitable for measuring cytosolic [Ca2+] after cell stimulation in a range from 0.5 to 10, it cannot be used in organelles where [Ca2+] is much higher, such as in the lumen of endoplasmic/sarcoplasmic reticulum (ER/SR) and mitochondria. However, some modifications made on aequorin itself or on coelenterazine, its lipophilic prosthetic luminophore, and the addition of targeting sequences or the fusion with resident proteins allowed the specific organelle localization and the measurements of intra-organelle Ca2+ levels. In the last years, the development of multiwell plate readers has opened the possibility to perform aequorin-based high-throughput screenings and has overcome some limitation of the standard method. Here we present the procedure for expressing, targeting, and reconstituting aequorin in intact cells and for measuring Ca2+ in the bulk cytosol, mitochondria, and ER by a high-throughput screening system. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Synthetic Route of 55779-48-1

The Article related to calcium cytosol mitochondria endoplasmic reticulum photoluminescence probe, aequorin, calcium, calcium probes, cytosol, er, high-throughput screening, mitochondria, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Synthetic Route of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On May 17, 2007, Chen, Xin; Coate, Heather; Crew, Andrew Philip; Dong, Han-Qing; Honda, Ayako; Mulvihill, Mark Joseph; Tavares, Paula A.R.; Wang, Jing; Werner, Douglas S.; Mulvihill, Kristen Michelle; Siu, Kam W.; Panicker, Bijoy; Bharadwaj, Apoorba; Arnold, Lee D.; Jin, Meizhong; Volk, Brian; Weng, Qinghua; Beard, James David published a patent.Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone The title of the patent was Preparation of substituted imidazopyrazines and related compounds as mTOR inhibitors. And the patent contained the following:

The title compounds I [X1, X2 = N or C(E1)aa; X5 = N, C(E1)aa or N(E1)aa; X3, X4, X6, X7 = N or C, wherein at least one of X3-X7 = N or N(E1)aa; R3 = alkyl, cycloalkyl, aryl, etc.; Q1 = (un)substituted indolyl, benzothiazolyl, etc.; E1 = halo, CF3, OCF3, etc.; aa = 0-1; with provisos] that are inhibitors of mTOR useful in the treatment of cancer, were prepared and formulated. Thus, coupling 8-amino-3-cyclobutyl-1-iodoimidazo[3,4-a]pyrazine with 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole afforded II. The exemplified compounds I showed activity against mTOR kinase as demonstrated in the assays described in this invention. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

The Article related to imidazopyrazine preparation mtor frap protein kinase inhibitor antitumor, imidazotriazine preparation mtor frap protein kinase inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On September 3, 2020, Chen, Yi published a patent.Category: pyrazines The title of the patent was Preparation of pyrrolopyrazines and related heterocycles as inhibitors of BTK and mutants thereof for the treatment of neoplastic, autoimmune and inflammatory disorders. And the patent contained the following:

The invention relates to preparation of pyrrolopyrazines and related heterocycles as inhibitors of BTK and mutants thereof. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compds and pharmaceutical compositions with them. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Category: pyrazines

The Article related to pyrrolopyrazine preparation prodrug pharmaceutical anticancer immunomodulator antiinflammatory, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On November 30, 2020, Krasitskaya, V. V.; Bashmakova, E. E.; Kudryavtsev, A. N.; Vorobjeva, M. A.; Shatunova, E. A.; Frank, L. A. published an article.Category: pyrazines The title of the article was The Hybrid Protein ZZ-OL as an Analytical Tool for Biotechnology Research. And the article contained the following:

Abstract: The gene of the hybrid protein that encodes the double synthetic fragment proZZ of the Ig-binding domain of protein A of Staphylococcus aureus and apo-obelin joined by a short linker has been cloned. The corresponding hybrid protein has been obtained by expression in Escherichia coli cells. The protein activated with a substrate (coelenterazine) possesses the bioluminescent Ca2+-dependent activity of the photoprotein close to that of recombinant wild-type obelin, and the Ig-binding ability of protein A. It has been shown that the hybrid can be used as a highly sensitive label to detect antibodies and estimate their affinity and interaction with recombinant proteins, as well as in investigations of other kinds. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Category: pyrazines

The Article related to staphylococcus escherichia hybrid protein zz ol biotechnol research, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On November 19, 2009, Crew, Andrew P.; Jin, Meizhong; Kadalbajoo, Mridula; Kleinberg, Andrew; Mulvihill, Mark J.; Wang, Jing published a patent.Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone The title of the patent was Substituted imidazopyrazines and imidazotriazines as ACK1 inhibitors and their preparation. And the patent contained the following:

The invention relates to fused pyridine-based bicyclic compounds having the structure of formula I, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. Compounds of formula I wherein A is CH and N; Q1 is X1Y1Z1, 1-phenylbenzimidazol-5-yl and carbazolyl; X1 is (un)substituted 5- to 10-membered cyclic ring; Y is CO, O, S, SO, SO2, etc.; Z1 is (un)substituted 5- to 10-membered cyclic ring and C1-6 alkoxy; R1 is SH and derivatives, (un)substituted C1-6 alkyl, (un)substituted 5,6-bicyclic aryl and (un)substituted 3- to 6-membered ring; and pharmaceutically acceptable salt thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their ACK1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.1759 μM. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

The Article related to imidazopyrazine imidazotriazine preparation ack1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On December 31, 2020, Rodriguez-Rodriguez, Ismael; Kalafut, Joanna; Czerwonka, Arkadiusz; Rivero-Muller, Adolfo published an article.Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one The title of the article was A novel bioassay for quantification of surface Cannabinoid receptor 1 expression. And the article contained the following:

The cannabinoid receptor type 1 (CB1) plays critical roles in multiple physiol. processes such as pain perception, brain development and body temperature regulation. Mutations on this gene (CNR1), results in altered functionality and/or biosynthesis such as reduced membrane expression, changes in mRNA stability or changes in downstream signaling that act as triggers for diseases such as obesity, Parkinson, Huntington, among others; thus, it is considered as a potential pharmacol. target. To date, multiple quantification methods have been employed to determine how these mutations affect receptor expression and localization; however, they present serious disadvantages that may arise quantifying errors. Here, we describe a sensitive bioassay to quantify receptor surface expression; in this bioassay the Gaussia Luciferase (GLuc) was fused to the extracellular portion of the CB1. The GLuc activity was assessed by coelenterazine addition to the medium followed by immediate readout. Based on GLuc activity assay, we show that the GLuc signals corelate with CB1 localization, besides, we showed the assay functionality and reliability by comparing its results with those generated by previously reported mutations on the CNR1 gene and by using flow cytometry to determine the cell surface receptor expression. Detection of membrane-bound CB1, and potentially other GPCRs, is able to quickly screen for receptor levels and help to understand the effect of clin. relevant mutations or polymorphisms. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

The Article related to cnr1 surface receptor luciferase mutation bioassay, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On January 2, 2014, Do, Steven; Hu, Huiyong; Kolesnikov, Aleksandr; Tsui, Vickie H.; Wang, Xiaojing published a patent.SDS of cas: 87486-34-8 The title of the patent was 5-Azaindazole compounds as Pim kinase inhibitors and their preparation. And the patent contained the following:

5-Azaindazole compounds of formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Compounds of formula I wherein R1 is (un)substituted 5- to 6-membered heteroaryl; R2 is (un)substituted Ph and (un)substituted 6-membered heteroaryl; and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their Pim kinase inhibitory activity (data given). The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).SDS of cas: 87486-34-8

The Article related to azaindazole preparation pim kinase inhibitors, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Larionova, Marina D.; Markova, Svetlana V.; Tikunova, Nina V.; Vysotski, Eugene S. published an article in 2020, the title of the article was The smallest isoform of Metridia longa luciferase as a fusion partner for hybrid proteins.Electric Literature of 55779-48-1 And the article contains the following content:

Bioluminescent proteins are widely used as reporter mols. in various in vitro and in vivo assays. The smallest isoform of Metridia luciferase (MLuc7) is a highly active, naturally secreted enzyme which, along with other luciferase isoforms, is responsible for the bright bioluminescence of marine copepod Metridia longa. In this study, we report the construction of two variants of a hybrid protein consisting of MLuc7 and 14D5a single-chain antibody to the surface glycoprotein E of tick-borne encephalitis virus as a model fusion partner. We demonstrate that, whereas fusion of a single-chain antibody to either N- or C-terminus of MLuc7 does not affect its bioluminescence properties, the binding site on the single-chain antibody influences its binding capacity. The affinity of 14D5a-MLuc7 hybrid protein (KD = 36.2 nM) where the C-terminus of the single-chain antibody was fused to the N-terminus of MLuc7, appeared to be 2.5-fold higher than that of the reverse, MLuc7-14D5a (KD = 87.6 nM). The detection limit of 14D5a-MLuc7 hybrid protein was estimated to be 45 pg of the recombinant glycoprotein E. Although the smallest isoform of M. longa luciferase was tested as a fusion partner only with a single-chain antibody, it is reasonable to suppose that MLuc7 can also be successfully used as a partner for genetic fusion with other proteins. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Electric Literature of 55779-48-1

The Article related to metridia longa luciferase fusion hybrid protein, bioluminescence, coelenterazine, copepod luciferase, immunoassay, single-chain antibody, tick-borne encephalitis virus, Nonmammalian Biochemistry: Classical Genetics and Phylogeny and other aspects.Electric Literature of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Vicente, Manuel; Salgado-Almario, Jussep; Collins, Michelle M.; Martinez-Sielva, Antonio; Minoshima, Masafumi; Kikuchi, Kazuya; Domingo, Beatriz; Llopis, Juan published an article in 2021, the title of the article was Cardioluminescence in Transgenic Zebrafish Larvae: A Calcium Imaging Tool to Study Drug Effects and Pathological Modeling.Synthetic Route of 55779-48-1 And the article contains the following content:

Zebrafish embryos and larvae have emerged as an excellent model in cardiovascular research and are amenable to live imaging with genetically encoded biosensors to study cardiac cell behaviors, including calcium dynamics. To monitor calcium ion levels in three to five days post-fertilization larvae, we have used bioluminescence. We generated a transgenic line expressing GFP-aequorin in the heart, Tg(myl7:GA), and optimized a reconstitution protocol to boost aequorin luminescence. The analog diacetylh-coelenterazine enhanced light output and signal-to-noise ratio. With this cardioluminescence model, we imaged the time-averaged calcium levels and beat-to-beat calcium oscillations continuously for hours. As a proof-of-concept of the transgenic line, changes in ventricular calcium levels were observed by Bay K8644, an L-type calcium channel activator and with the blocker nifedipine. The β-adrenergic blocker propranolol decreased calcium levels, heart rate, stroke volume, and cardiac output, suggesting that larvae have a basal adrenergic tone. Zebrafish larvae treated with terfenadine for 24 h have been proposed as a model of heart failure. Tg(myl7:GA) larvae treated with terfenadine showed bradycardia, 2:1 atrioventricular block, decreased time-averaged ventricular calcium levels but increased calcium transient amplitude, and reduced cardiac output. As alterations of calcium signalling are involved in the pathogenesis of heart failure and arrhythmia, the GFP-aequorin transgenic line provides a powerful platform for understanding calcium dynamics. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Synthetic Route of 55779-48-1

The Article related to zebrafish calcium aequorin coelenterazine heart failure imaging, aequorin, calcium, coelenterazine, heart, heart failure, imaging, zebrafish, Nonmammalian Biochemistry: Classical Genetics and Phylogeny and other aspects.Synthetic Route of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Jaiswal, Poonam B.; Tung, Jack K.; Gross, Robert E.; English, Arthur W. published an article in 2020, the title of the article was Motoneuron activity is required for enhancements in functional recovery after peripheral nerve injury in exercised female mice.Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one And the article contains the following content:

Inhibitory luminopsins (iLMO2) integrate opto- and chemo-genetic approaches and allow for cell-type specific inhibition of neuronal activity. When exposed to a Renilla luciferase substrate, Coelenterazine (CTZ), iLMO2 generates bioluminescence-mediated activation of its amino-terminal halorhodopsin, resulting in neuronal inhibition. Moderate daily exercise in the form of interval treadmill-training (IT) applied following a peripheral nerve injury results in enhanced motor axon regeneration and muscle fiber reinnervation in female mice. We hypothesized that iLMO2 mediated inhibition of motoneuron activity during IT would block this enhancement. Unilateral i.m. injections of Cre-dependent AAV2/9-EF1a-DIO-iLMO2 (∼8.5 x 1013 vg/mL) were made into the gastrocnemius and tibialis anterior muscles of young female ChAT-IRES-Cre mice, thereby limiting iLMO2 expression specifically to their motoneurons. Four to six weeks were allowed for retrograde viral transduction after which a unilateral sciatic nerve transection (Tx) and repair was performed. Animals were randomized into four groups: IT only, IT + CTZ, CTZ only, and untreated (UT). Three weeks post Tx-repair, the maximal amplitude direct muscle responses (M-max) in both muscles in the IT only group were significantly greater than in UT mice, consistent with the enhancing effects of this exercise regimen. Inhibiting motoneuron activity during exercise by a single injection of CTZ, administered 30 min prior to exercise, completely blocked the enhancing effect of exercise. Similar treatments with CTZ in mice without iLMO2 had no effect on regeneration. Neuronal activity is required for successful enhancement of motor axon regeneration by exercise. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

The Article related to exercise nerve injury female, rrid:cvcl_0045, rrid:mgi:3689725, inhibitory luminopsin, m-response, motoneuron activity, sciatic nerve injury, treadmill training, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem