Category: 51047-56-4

HPLC of Formula: C8H12N4, The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states.

A series of pyridazinylpiperazines were synthesized and evaluated for VR1 antagonist activity in order to improve upon the pharmaceutical and pharmacological properties of BCTC. A structurally biased chemical library of pyridazinylpiperazine analogs was prepared in an effort to improve the pharmaceutical and pharmacological profile of the lead compound N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H) -carboxamide (BCTC). The library was evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH 5.5-induced (pH) FLIPR assays in a human VR1-expressing HEK293 cell line. The most potent VR1 antagonists were found to have IC50 values in the range of 9-200 nM with improved pharmaceutical and pharmacological profiles versus the lead BCTC. These compounds represent possible second-generation BCTC analogs.

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 51047-56-4 is helpful to your research. HPLC of Formula: C8H12N4

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Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment. Electric Literature of 51047-56-4

DMPP is a well-known nicotinic agonist that does not fit any proposed pharmacophore for nicotinic binding and represents a unique ligand among the hundreds of nicotinic agonists studied in the past decades. A systematic modulation of the chemical structure of DMPP, aimed to establish its structure-affinity relationships, is reported. The research has allowed to identify molecules such as 11c, 13c, 14c, and 28c, with affinities for alpha4beta2 receptors in the low nanomolar range, some 2 orders of magnitude lower than the lead compound. The agonistic properties of the most interesting compounds have been assessed by measuring their analgesic activity on mice (hot-plate test). Another result of the research was the identification of DMPP analogues, such as 3a (Ki = 90 nM) and 14b (Ki = 180 nM), that maintain affinity for the central nicotinic receptor when the ammonium function is changed into an aminic one and are therefore possible leads for drug development in neurodegenerative diseases.

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 3-Piperazin-1-yl-pyridazine, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent，Which mentioned a new discovery about 51047-56-4

The present invention relates to bis-heteroaryl compounds of formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson’s disease, Alzheimer’s disease, Lewy body disease, Parkinson’s disease with dementia, fronto-temporal dementia, Huntington’s Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.

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A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC50=2 muM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (IC50<20 nM). Additionally, physicochemical and pharmacokinetic properties were evaluated. It could be shown that compounds bearing a piperazine or phenyl substituted betaAla-Gly side chain exhibited the best overall profile. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Recommanded Product: 3-Piperazin-1-yl-pyridazine, you can also check out more blogs about51047-56-4

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2223 – PubChem

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 51047-56-4, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 51047-56-4, Name is 3-Piperazin-1-yl-pyridazine, molecular formula is C8H12N4

A series of pyridazinylpiperazines were synthesized and evaluated for VR1 antagonist activity in order to improve upon the pharmaceutical and pharmacological properties of BCTC. A structurally biased chemical library of pyridazinylpiperazine analogs was prepared in an effort to improve the pharmaceutical and pharmacological profile of the lead compound N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H) -carboxamide (BCTC). The library was evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH 5.5-induced (pH) FLIPR assays in a human VR1-expressing HEK293 cell line. The most potent VR1 antagonists were found to have IC50 values in the range of 9-200 nM with improved pharmaceutical and pharmacological profiles versus the lead BCTC. These compounds represent possible second-generation BCTC analogs.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2224 – PubChem

 

Electric Literature of 51047-56-4, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 51047-56-4, Name is 3-Piperazin-1-yl-pyridazine, molecular formula is C8H12N4. In a Article，once mentioned of 51047-56-4

DMPP is a well-known nicotinic agonist that does not fit any proposed pharmacophore for nicotinic binding and represents a unique ligand among the hundreds of nicotinic agonists studied in the past decades. A systematic modulation of the chemical structure of DMPP, aimed to establish its structure-affinity relationships, is reported. The research has allowed to identify molecules such as 11c, 13c, 14c, and 28c, with affinities for alpha4beta2 receptors in the low nanomolar range, some 2 orders of magnitude lower than the lead compound. The agonistic properties of the most interesting compounds have been assessed by measuring their analgesic activity on mice (hot-plate test). Another result of the research was the identification of DMPP analogues, such as 3a (Ki = 90 nM) and 14b (Ki = 180 nM), that maintain affinity for the central nicotinic receptor when the ammonium function is changed into an aminic one and are therefore possible leads for drug development in neurodegenerative diseases.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 51047-56-4. In my other articles, you can also check out more blogs about 51047-56-4

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2222 – PubChem

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Product Details of 51047-56-4, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 51047-56-4, Name is 3-Piperazin-1-yl-pyridazine, molecular formula is C8H12N4

The present invention provides compounds, compositions thereof, and methods of using the same.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Product Details of 51047-56-4, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 51047-56-4, in my other articles.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2219 – PubChem

 

Electric Literature of 51047-56-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.51047-56-4, Name is 3-Piperazin-1-yl-pyridazine, molecular formula is C8H12N4. In a Article，once mentioned of 51047-56-4

A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D 4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin- 1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 mumol/kg, with a positive response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D 4 selective agonism in this series of analogues.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2220 – PubChem

 

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New arylpiperazine derivatives as antagonists of the human cloned 5-HT4 receptor isoforms

New derivatives of arylpiperazine 9 were designed from ML 10302, a potent 5-HT4 receptor agonist in the gastrointestinal system. Compounds were synthesized by condensation of a number of available arylpiperazines or heteroarylpiperazines with 2-bromoethyl 4-amino-5-chloro-2-methoxybenzoate. They were evaluated in binding assays on the recently cloned human 5-HT(4(e)) isoform stably expressed in C6 glial cells with [3H]GR 113808 as the radioligand. The affinity values (K(i)) depended upon the substituent on the aromatic ring. A chlorine atom produced a marked drop in activity (K(i) > 100 nM), while a m-methoxy group gave a compound with nanomolar affinity (K(i) = 3 nM). The most potent compounds were the heterocyclic derivatives with pyrimidine, pyrazine, pyridazine, or pyridine moieties (compounds 9r, 9t, 9u, 9x, respectively). K(i) values for 9a and 9r were determined for the 5-HT(4(a)), 5-HT(4(b)), 5-HT(4(c)), and 5-HT(4(d)) receptor isoforms transiently expressed in COS cells. The results indicated that the compounds were not selective. They produced an inhibition of the 5-HT-stimulated cyclic AMP synthesis in the C6 glial cells stably expressing the 5-HT(4(e)) receptor and shifted the 5-HT concentration-effect curve on adenylyl cyclase activity with pK(D) values of 7.44 and 8.47, respectively. In isolated human atrial myocytes, 9r antagonized the stimulatory effect of 5-HT on the L-type calcium current (I(Ca)) with a K(D) value of 0.7 nM.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2221 – PubChem

 

51047-56-4, Name is 3-Piperazin-1-yl-pyridazine, belongs to pyridazine compound, is a common compound. Application In Synthesis of 3-Piperazin-1-yl-pyridazineIn an article, once mentioned the new application about 51047-56-4.

Aryl carbamate derivatives, preperation and use thereof

The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.

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