Discovery of 98006-90-7

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Zhuang, Linghang; Tice, Colin M.; Xu, Zhenrong; Zhao, Wei; Cacatian, Salvacion; Ye, Yuan-Jie; Singh, Suresh B.; Lindblom, Peter; McKeever, Brian M.; Krosky, Paula M.; Zhao, Yi; Lala, Deepak; Kruk, Barbara A.; Meng, Shi; Howard, Lamont; Johnson, Judith A.; Bukhtiyarov, Yuri; Panemangalore, Reshma; Guo, Joan; Guo, Rong; Himmelsbach, Frank; Hamilton, Bradford; Schuler-Metz, Annette; Schauerte, Heike; Gregg, Richard; McGeehan, Gerard M.; Leftheris, Katerina; Claremon, David A. researched the compound: 2-Bromo-5-methylpyrazine( cas:98006-90-7 ).Quality Control of 2-Bromo-5-methylpyrazine.They published the article 《Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor》 about this compound( cas:98006-90-7 ) in Bioorganic & Medicinal Chemistry. Keywords: BI135585 oxazinanone hydroxysteroid dehydrogenase inhibitor; 11beta hydroxysteroid dehydrogenase type 1; Human adipocyte; Human adipose tissue; Inhibitor; Oxazinanone. We’ll tell you more about this compound (cas:98006-90-7).

A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (I) has been identified. Compound I inhibited 11β HSD1 activity in human adipocytes with an IC50 of 4.3 nM and in primary human adipose tissue with an IC80 of 53 nM. Oral administration of I to cynomolgus monkey inhibited 11β HSD1 activity in adipose tissue. Compound I exhibited >1000× selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clin. trials in 2011.

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

Why do aromatic interactions matter of compound: 98006-90-7

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Recommanded Product: 2-Bromo-5-methylpyrazine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-Bromo-5-methylpyrazine, is researched, Molecular C5H5BrN2, CAS is 98006-90-7, about Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.

Recent findings showing a relation between mutations in the NaV1.7 channel in humans and altered pain sensation has contributed to increase the attractiveness of this ion channel as target for development of potential analgesics. Amido chromanes 1 and 2 were identified as blockers of the NaV1.7 channel and analogs with modifications of the 5-substituent and the carboxamide part of the mol. were prepared to establish the structure-activity relationship. Compounds 13 and 29 with good overall in vitro and in vivo rat PK profile were identified. Furthermore, 29 showed in vivo efficacy in a nociceptive pain model.

Here is a brief introduction to this compound(98006-90-7)Recommanded Product: 2-Bromo-5-methylpyrazine, if you want to know about other compounds related to this compound(98006-90-7), you can read my other articles.

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