Glucokinase-Activators-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html GlucokinaseHexokinase IV; Hexokinase DGlucokinase is an enzyme that facilitates phosphorylation of glucose to glucose-6-phosphate. Glucokinase occurs in cells in theliver,pancreas, gut, and brain of humans and most other vertebrates. In each of

2、 these organs it plays an important role in the regulationof carbohydrate metabolism by acting as a glucose sensor, triggering shifts in metabolism or cell function in response to rising orfalling levels of glucose, such as occur after a meal or when fasting. Glucokinase has a lower affinity for glu

3、cose than the otherhexokinases do, and its activity is localized to a few cell types, leaving the other three hexokinases as more important preparers ofglucose for glycolysis and glycogen synthesis for most tissues and organs. Mutations of the gene for this enzyme can cause unusualforms of diabetes

4、or hypoglycemia.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html Glucokinase HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html HYPERLINK https:/www.MedC

5、hemE/Targets/Glucokinase.html Activators HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html & HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html HYPERLINK https:/www.MedChemE/Targets/Glucokinase.html Modulators HYPERLINK https:/www.MedCh

6、emE/AM-2394.html AM-2394 HYPERLINK https:/www.MedChemE/AM-2394.html HYPERLINK https:/www.MedChemE/amg-1694.html AMG-1694Cat. No.: HY-100221 Cat. No.: HY-12614AM-2394 is a structurally distinct glucokinaseactivator (GKA). AM-2394 activates glucokinase(GK) with an EC of 60 nM.50AMG-1694 is a potent gl

7、ucokinaseglucokinaseregulatory protein (GK-GKRP) disruptors andpromotes the dissociation of the GK-GKRP complexwith an IC of 7 nM, indirectly increasing GK50enzymatic activity.Purity: 99.48%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development

8、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AMG-3969.html AMG-3969 HYPERLINK https:/www.MedChemE/AMG-3969.html HYPERLINK https:/www.MedChemE/ar453588.html AR453588Cat. No.: HY-12411 Cat. No.: HY-133127AMG-3969 is a potent glucokinase-glucokinaseregulatory protein interaction (GK-GKRP)dis

9、ruptor with an IC of 4 nM.50AR453588 is a potent and orally bioavailableanti-diabetic glucokinase activator, with an EC50of 42 nM. AR453588 shows anti-hyperglycemicactivity.Purity: 99.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.69%Clinical Da

10、ta: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ar453588-hydrochloride.html AR453588 HYPERLINK https:/www.MedChemE/ar453588-hydrochloride.html HYPERLINK https:/www.MedChemE/ar453588-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/ar4535

11、88-hydrochloride.html HYPERLINK https:/www.MedChemE/azd1656.html AZD1656Cat. No.: HY-133127A Cat. No.: HY-15675AR453588 hydrochloride is a potent and orallybioavailable anti-diabetic glucokinase activator,with an EC of 42 nM. AR453588 hydrochloride50shows anti-hyperglycemic activity.AZD1656 is a pot

12、ent, selective and orally activeglucokinase activator with an EC of 60 nM.50AZD1656 has the potential for type 2 diabetesresearch.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/bms-8

13、20132.html BMS-820132 HYPERLINK https:/www.MedChemE/bms-820132.html HYPERLINK https:/www.MedChemE/dorzagliatin.html DorzagliatinCat. No.: HY-144289(HMS5552) Cat. No.: HY-109030BMS-820132 is a partial glucokinase activator witha AC of 29 nM.50Dorzagliatin (HMS5552), a dual-acting glucokinase(GK) acti

14、vator, improves glycaemic control andpancreatic -cell function in type 2 diabetes.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gka50.html GKA50 HY

15、PERLINK https:/www.MedChemE/gka50.html HYPERLINK https:/www.MedChemE/gka50-quarterhydrate.html GKA50 HYPERLINK https:/www.MedChemE/gka50-quarterhydrate.html HYPERLINK https:/www.MedChemE/gka50-quarterhydrate.html quarterhydrateCat. No.: HY-15671 Cat. No.: HY-15671AGKA50 is a potent glucokinase activ

16、ator (EC =3350nM at 5 mM glucose). GKA50 stimulates insulinrelease from mouse islets of Langerhans. GKA50 isa glucose-like activator of beta-cell metabolismin rodent and human islets and a Ca2+-dependentmodulator of insulin secretion.GKA50 quarterhydrate is a potent glucokinaseactivator (EC =33 nM a

17、t 5 mM glucose) and50stimulates insulin release from mouse islets ofLangerhans.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:

18、/www.MedChemE/LY2608204.html Globalagliatin(LY2608204) Cat. No.: HY-13529 HYPERLINK https:/www.MedChemE/Glucokinase_activator_1.html Glucokinase HYPERLINK https:/www.MedChemE/Glucokinase_activator_1.html HYPERLINK https:/www.MedChemE/Glucokinase_activator_1.html activator HYPERLINK https:/www.MedChe

19、mE/Glucokinase_activator_1.html HYPERLINK https:/www.MedChemE/Glucokinase_activator_1.html 1Cat. No.: HY-101788Globalagliatin (LY2608204) is a activator ofglucokinase (GK) with EC50 of 42 nM.Glucokinase activator 1 is a liver-directedglucokinase activator with an EC of 34 nM.50Purity: 98.0%Clinical

20、Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/glucokinase-activator-3.html Glucokinase HYPERLINK https:/www.MedChemE/glucokinase-activator-3.html HYPERLINK https:/www.MedChemE/glucokinase-activ

21、ator-3.html activator HYPERLINK https:/www.MedChemE/glucokinase-activator-3.html HYPERLINK https:/www.MedChemE/glucokinase-activator-3.html 3 HYPERLINK https:/www.MedChemE/glucokinase-activator-3.html HYPERLINK https:/www.MedChemE/ihvr-11029.html IHVR-11029Cat. No.: HY-144287 Cat. No.: HY-117721Gluc

22、okinase activator 3 is a potent and fullGlucokinase (GK) activator with an AC of 3850nM. Glucokinase activator 3 has the potential forthe research of type 2 diabetes.IHVR-11029 is a small molecule inhibitor of ER-glucosidases, with an EC of 0.09 M.50Purity: 98%Clinical Data: No Development ReportedS

23、ize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mk-0941.html MK-0941 HYPERLINK https:/www.MedChemE/mk-0941.html HYPERLINK https:/www.MedChemE/mk-0941-free-base.html MK-0941 HYPERLINK https:/www.MedChemE/mk-0941-free-base.html HYPERLINK h

24、ttps:/www.MedChemE/mk-0941-free-base.html free HYPERLINK https:/www.MedChemE/mk-0941-free-base.html HYPERLINK https:/www.MedChemE/mk-0941-free-base.html baseCat. No.: HY-19843 Cat. No.: HY-19843AMK-0941 is a potent, orally active and allostericglucokinase activator, with EC s of 240 and 6550nM for r

25、ecombinant human glucokinase in thepresence of 2.5 and 10 mM glucose, respectively.MK-0941 has potential in the treatment of type 2diabetes.MK-0941 free base is an orally active glucokinaseactivator, with EC s of 240 and 65 nM for50recombinant human glucokinase in the presence of2.5 and 10 mM glucos

26、e, respectively.Purity: 98.84%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Palmitelaidic_Acid.html Palmitelaidic HYPERLINK https:/www.MedChemE/Palmitelaidic_Acid.html HYPERLINK https:/www.MedC

27、hemE/Palmitelaidic_Acid.html Acid HYPERLINK https:/www.MedChemE/Palmitelaidic_Acid.html HYPERLINK https:/www.MedChemE/palmitelaidic-acid-d13.html Palmitelaidic HYPERLINK https:/www.MedChemE/palmitelaidic-acid-d13.html HYPERLINK https:/www.MedChemE/palmitelaidic-acid-d13.html acid-d13(9-trans-Hexadec

28、enoic acid; trans-Palmitoleic acid) Cat. No.: HY-N2341Cat. No.: HY-N2341SPalmitelaidic Acid (9-trans-Hexadecenoic acid) isthe trans isomer of palmitoleic acid. Palmitoleicacid is one of the most abundant fatty acids inserum and tissue.Palmitelaidic acid-d13 is the deuterium labeledPalmitelaidic Acid

29、. Palmitelaidic Acid(9-trans-Hexadecenoic acid) is the trans isomer ofpalmitoleic acid. Palmitoleic acid is one of themost abundant fatty acids in serum and tissue.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mg (393 mM * 100 L in Ethanol),Purity: 98%Clinical Data: No Development Repo

30、rtedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pf-04937319.html PF-04937319 HYPERLINK https:/www.MedChemE/pf-04937319.html HYPERLINK https:/www.MedChemE/PF-04991532.html PF-04991532Cat. No.: HY-108328 Cat. No.: HY-100181PF-04937319 is a glucokinase activator (GKA) withEC value of 154.4 M, one of the most50promising strategies for the treatment of type 2diabetes mellitus.PF-04991532 is a potent, hepatoselectiveglucokinase act