Pharmacological evaluation of HM41322, a novel SGLT1/2 dual inhibitor, in vitro and in vivo
DC Field | Value | Language |
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dc.contributor.author | Lee, Kyu Hang | - |
dc.contributor.author | Lee, Sang Don | - |
dc.contributor.author | Kim, Namdu | - |
dc.contributor.author | Suh, Kwee Hyun | - |
dc.contributor.author | Kim, Young Hoon | - |
dc.contributor.author | Sim, Sang Soo | - |
dc.date.available | 2019-05-28T02:47:04Z | - |
dc.date.issued | 2019-01 | - |
dc.identifier.issn | 1226-4512 | - |
dc.identifier.issn | 2093-3827 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/18366 | - |
dc.description.abstract | HM41322 is a novel oral sodium-glucose cotransporter (SGLT) 1/2 dual inhibitor. In this study, the in vitro and in vivo pharmacokinetic and pharmacologic profiles of HM41322 were compared to those of dapagliflozin. HM41322 showed a 10-fold selectivity for SGLT2 over SGLT1. HM41322 showed an inhibitory effect on SGLT2 similar to dapagliflozin, but showed a more potent inhibitory effect on SGLT1 than dapagliflozin. The maximum plasma HM41322 level after single oral doses at 0.1, 1, and 3 mg/kg were 142, 439, and 1830 ng/ml, respectively, and the T-1/2 was 3.1 h. HM41322 was rapidly absorbed and reached the circulation within 15 min. HM41322 maximized urinary glucose excretion by inhibiting both SGLT1 and SGLT2 in the kidney. HM41322 3 mg/kg caused the maximum urinary glucose excretion in normoglycemic mice (19.32 +/- 1.16 mg/g) at 24 h. In normal and diabetic mice, HM41322 significantly reduced glucose excursion. Four-week administration of HM41322 in db/db mice reduced HbA1c in a dose dependent manner. Taken together, HM41322 showed a favorable preclinical profile of postprandial glucose control through dual inhibitory activities against SGLT1 and SGLT2. | - |
dc.format.extent | 8 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY | - |
dc.title | Pharmacological evaluation of HM41322, a novel SGLT1/2 dual inhibitor, in vitro and in vivo | - |
dc.type | Article | - |
dc.identifier.doi | 10.4196/kjpp.2019.23.1.55 | - |
dc.identifier.bibliographicCitation | KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY, v.23, no.1, pp 55 - 62 | - |
dc.identifier.kciid | ART002432162 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000454432300006 | - |
dc.identifier.scopusid | 2-s2.0-85060142302 | - |
dc.citation.endPage | 62 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 55 | - |
dc.citation.title | KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY | - |
dc.citation.volume | 23 | - |
dc.type.docType | Article | - |
dc.publisher.location | 대한민국 | - |
dc.subject.keywordAuthor | Dapagliflozin | - |
dc.subject.keywordAuthor | Diabetes mellitus | - |
dc.subject.keywordAuthor | HM41322 | - |
dc.subject.keywordAuthor | SGLT1/2 dual inhibitor | - |
dc.subject.keywordPlus | GLUCOSE COTRANSPORTER SGLT1 | - |
dc.subject.keywordPlus | IMPROVED GLYCEMIC CONTROL | - |
dc.subject.keywordPlus | ABSORPTION | - |
dc.subject.keywordPlus | LX4211 | - |
dc.subject.keywordPlus | COMPLICATIONS | - |
dc.subject.keywordPlus | 30-50-PERCENT | - |
dc.subject.keywordPlus | REABSORPTION | - |
dc.subject.keywordPlus | HOMEOSTASIS | - |
dc.subject.keywordPlus | TRANSPORT | - |
dc.subject.keywordPlus | GLP-1 | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Physiology | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Physiology | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
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