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產(chǎn)品名稱

APD 668 - JNJ 28630368

產(chǎn)品貨號(hào)

Axon 2380 CAS [832714-46-2] MF C21H24FN5O5SMW 477.51 Purity: 100% Soluble in DMSO Description Potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM). References Certificates Categories Extra info G. Semple et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg. Med. Chem. Lett. 2011, 21, 3134-3141. ? M. Sakairi et al. Synthesis and pharmacological profile of a new selective G protein-coupled receptor 119 agonist; 6-((2-fluoro-3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propyl)amino)-2,3-dihydro.... Chem. Pharm. Bull. 2012, 60, 1093-1095. ? E. Weisberg et al. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013, 8, e56473. Certificate of Analysis Material Safety Data Sheet CNS Diabetes & Metabolism Endocrinology GPR119 A15 Potent and selective, orally active GPR119 agonist Chemical name isopropyl 4-(1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate Parent CAS No. [832714-46-2] Order Size Unit Price Stock 5 mg €125.00 In Stock

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現(xiàn)貨詢價(jià)，電話：010-67529703

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產(chǎn)品品牌

axonmedchem

產(chǎn)品概述

產(chǎn)品詳情

APD 668 - JNJ 28630368

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 2380

CAS [832714-46-2]

MF C21H24FN5O5S
MW 477.51

Purity: 100%
Soluble in DMSO

APD 668

Description

Potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat.
APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).

G. Semple et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg. Med. Chem. Lett. 2011, 21, 3134-3141.

M. Sakairi et al. Synthesis and pharmacological profile of a new selective G protein-coupled receptor 119 agonist; 6-((2-fluoro-3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propyl)amino)-2,3-dihydro.... Chem. Pharm. Bull. 2012, 60, 1093-1095.

E. Weisberg et al. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013, 8, e56473.

Certificate of Analysis
Material Safety Data Sheet

CNS Diabetes & Metabolism Endocrinology GPR119 A15

Potent and selective, orally active GPR119 agonist

Chemical name

isopropyl 4-(1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate

Parent CAS No.

[832714-46-2]

產(chǎn)品資料

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