Insulin-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Insulin HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html ReceptorInsulin receptor (IR), a phylogenetically ancient tyrosine kinase receptor, is a large cell surface gly

2、coprotein that concentrates insulinat the site of action and also initiates responses to insulin. The receptor is a disulfide-linked oligomer comprised of two alpha andtwo beta subunits. The insulin receptor exists in two isoforms, IR-A and IR-B, expressed in different relative abundance in thevario

3、us organs and tissues. The two IR isoforms have similar binding affinity for insulin but different affinity for insulin-like growthfactor (IGF)-2 and proinsulin, which are bound by IR-A but not IR-B.The insulin receptor has a crucial role in controlling glucose homeostasis, regulating lipid, protein

4、 and carbohydrate metabolism,and modulating brain neurotransmitter levels. Insulin receptor dysfunction has been associated with many diseases, includingdiabetes, cancer and Alzheimers disease.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Insulin HYPERLINK https:/www.Med

5、ChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYP

6、ERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/In

7、sulin Receptor.html Activators HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Insulin Receptor.html Modulators HYPERLINK https:

8、/www.MedChemE/AG1024.html AG1024(Tyrphostin AG 1024) Cat. No.: HY-10253 HYPERLINK https:/www.MedChemE/AGL-2263.html AGL-2263Cat. No.: HY-112720AG1024 (Tyrphostin AG 1024) is a reversible,competitive and selective IGF-1R inhibitor with anIC of 7 M. AG1024 inhibits phosphorylation of50 IR(IC50=57 M).

9、AG1024 induces apoptosis and hasanti-cancer activity.AGL-2263 is an insulin receptor and insulin-likegrowth factor (IGF) receptor inhibitor.Purity: 98.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 97.04%Clinical Data: No Development ReportedSize: 10 mM

10、1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/avj16.html AVJ16 HYPERLINK https:/www.MedChemE/avj16.html HYPERLINK https:/www.MedChemE/BMS-536924.html BMS-536924Cat. No.: HY-144873 Cat. No.: HY-10262AVJ16 is a member of the insulin-like growthfactor 2 mRNA-binding protein family. AVJ1

11、6regulates protein translation by binding to themRNAs of certain genes.BMS-536924 is an orally active, competitive andselective insulin-like growth factor receptor(IGF-1R) kinase and insulin receptor (IR) inhibitorwith IC s of 100 nM and 73 nM, respectively.50BMS-536924 has anti-cancer activity.Puri

12、ty: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BMS-754807.html BMS-754807Cat. No.: HY-10200 HYPERLINK https:/www.MedChemE/LDK378.html Ceritinib(LDK378) Cat. No

13、.: HY-15656BMS-754807 is a potent and reversible IGF-1R/IRinhibitor (IC =1.8 and 1.7 nM, respectively;50K=98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.83%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/da-jc4.html DA-JC4 HYPERL

14、INK https:/www.MedChemE/da-jc4.html HYPERLINK https:/www.MedChemE/demethylasterriquinone-b1.html Demethylasterriquinone HYPERLINK https:/www.MedChemE/demethylasterriquinone-b1.html HYPERLINK https:/www.MedChemE/demethylasterriquinone-b1.html B1Cat. No.: HY-P3255(DAQ B1; L-783281; Dimethylasterriquin

15、one) Cat. No.: HY-107586DA-JC4 is a dual GLP-1/GIP receptor agonist andcan be used for the research of neurologicaldisease and insulin signaling pathways.Demethylasterriquinone B1 is a selective insulinreceptor activator. Demethylasterriquinone B1stimulates tyrosine phosphorylation of the IR subunit

16、, and the activation of PIK3 and AKT.Purity: 96.57%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html GIP HYPERLINK https

17、:/www.MedChemE/gip-1-30-amide-porcine.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html (1-30) HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html amide, HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html HYPERLINK h

18、ttps:/www.MedChemE/gip-1-30-amide-porcine.html porcine HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html GIP HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.ht

19、ml (1-30) HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html amide, HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html porcine HYPERLINK https:/www.MedChe

20、mE/gip-1-30-amide-porcine-tfa.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-porcine-tfa.html TFACat. No.: HY-P2541 Cat. No.: HY-P2541AGIP (1-30) amide, porcine is a fullglucose-dependent insulinotropic polypeptide (GIP)receptor agonist with high affinity equal tonative GIP(1-42). GIP (1-30) amid

21、e, porcine is aweak inhibitor of gastric acid secretion andpotent stimulator of insulin.GIP (1-30) amide, porcine TFA is a fullglucose-dependent insulinotropic polypeptide (GIP)receptor agonist with high affinity equal tonative GIP(1-42). GIP (1-30) amide, porcine is aweak inhibitor of gastric acid

22、secretion andpotent stimulator of insulin.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.55%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/gip-1-30-amide-human.html GIP HYPERLINK https:/www.MedChemE/gip-1-30-amide-human.html HYPERLI

23、NK https:/www.MedChemE/gip-1-30-amide-human.html (1-30) HYPERLINK https:/www.MedChemE/gip-1-30-amide-human.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-human.html amide,human HYPERLINK https:/www.MedChemE/gip-1-30-amide-human.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html

24、GIP HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html (1-30) HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html amide,human HYPERLINK https:/www.

25、MedChemE/gip-1-30-amide-human-acetate.html HYPERLINK https:/www.MedChemE/gip-1-30-amide-human-acetate.html acetateCat. No.: HY-P2080 Cat. No.: HY-P2080BGIP (1-30) amide,human is a glucose-dependentinsulinotropic polypeptide (GIP) fragment. GIP isan incretin hormone that stimulates insulinsecretion a

26、nd reduces postprandial glycaemicexcursions.GIP (1-30) amide,human acetate is aglucose-dependent insulinotropic polypeptide (GIP)fragment. GIP is an incretin hormone thatstimulates insulin secretion and reducespostprandial glycaemic excursions.Purity: 98%Clinical Data: No Development ReportedSize: 1

27、 mg, 5 mgPurity: 98.26%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/gip-3-42-human.html GIP HYPERLINK https:/www.MedChemE/gip-3-42-human.html HYPERLINK https:/www.MedChemE/gip-3-42-human.html (3-42), HYPERLINK https:/www.MedChemE/gip-3-42-human.html HYP

28、ERLINK https:/www.MedChemE/gip-3-42-human.html humanCat. No.: HY-P2542 HYPERLINK https:/www.MedChemE/Gastric_Inhibitory_Peptide_GIP_,_human.html GIP, HYPERLINK https:/www.MedChemE/Gastric_Inhibitory_Peptide_GIP_,_human.html HYPERLINK https:/www.MedChemE/Gastric_Inhibitory_Peptide_GIP_,_human.html hu

29、man(Gastric Inhibitory Peptide (GIP), human) Cat. No.: HY-P0276GIP (3-42), human acts as a glucose-dependentinsulinotropic polypeptide (GIP) receptorantagonist, moderating the insulin secreting andmetabolic actions of GIP in vivo.GIP, human, a peptide hormone consisting of 42amino acids, is a stimul

30、ator of glucose-dependentinsulin secretion and a weak inhibitor of gastricacid secretion. GIP, human acts as an incretinhormone released from intestinal K cells inresponse to nutrient ingestion.Purity: 98.24%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No De

31、velopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/gip-human-tfa.html GIP, HYPERLINK https:/www.MedChemE/gip-human-tfa.html HYPERLINK https:/www.MedChemE/gip-human-tfa.html human HYPERLINK https:/www.MedChemE/gip-human-tfa.html HYPERLINK https:/www.MedChemE/gip-human-tfa.html TFA HYPER

32、LINK https:/www.MedChemE/gip-human-tfa.html HYPERLINK https:/www.MedChemE/GSK1838705A.html GSK1838705A(Gastric Inhibitory Peptide (GIP), human TFA) Cat. No.: HY-P0276ACat. No.: HY-13020GIP, human TFA, a peptide hormone consisting of 42amino acids, is a stimulator of glucose-dependentinsulin secretio

33、n and a weak inhibitor of gastricacid secretion. GIP, human TFA acts as an incretinhormone released from intestinal K cells inresponse to nutrient ingestion.GSK1838705A is a potent and reversible IGF-IR andthe insulin receptor inhibitor with IC s of 2.050and 1.6 nM, respectively. It also inhibits AL

34、Kwith an IC of 0.5 nM.50Purity: 96.24%Clinical Data: No Development ReportedSize: 1 mgPurity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GSK1904529A.html GSK1904529A HYPERLINK https:/www.MedChemE/GSK1904529A.html HYPERLINK h

35、ttps:/www.MedChemE/hnmpa.html HNMPACat. No.: HY-10524 Cat. No.: HY-101962GSK1904529A is a potent, selective, orally active,and ATP-competitive inhibitor of insulin-likegrowth factor-1 receptor (IGF-1R) and insulinreceptor (IR), with IC s of 27 and 25 nM,50respectively.HNMPA is a membrane impermeable

36、 insulin receptortyrosine kinase inhibitor. HNMPA inhibits serineand tyrosine autophosphorylation by the humaninsulin receptor. HNMPA has no effect on proteinkinase C or cyclic AMP-dependent protein kinaseactivities.Purity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg,

37、100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/hnmpa-am-3.html HNMPA-(AM)3 HYPERLINK https:/www.MedChemE/hnmpa-am-3.html HYPERLINK https:/www.MedChemE/Insulin_human_.html Insulin HYPERLINK https:/www.MedChemE/Insulin_human_.html H

38、YPERLINK https:/www.MedChemE/Insulin_human_.html (human)Cat. No.: HY-124097 Cat. No.: HY-P0035HNMPA-(AM)3 is a cell-permeable and selectiveinsulin receptor tyrosine kinase inhibitor analog ofHNMPA. HNMPA-(AM)3 greatly inhibits the ability ofprothoracicotropic hormone (PTTH) to activate ERKphosphoryl

39、ation and stimulate ecdysteroidogenesis.Insulin (human) is a polypeptide hormone thatregulates the level of glucose.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 96.90%Clinical Data: LaunchedSize: 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/insulin-glargine.html Ins

40、ulin HYPERLINK https:/www.MedChemE/insulin-glargine.html HYPERLINK https:/www.MedChemE/insulin-glargine.html glargine HYPERLINK https:/www.MedChemE/insulin-glargine.html HYPERLINK https:/www.MedChemE/Insulin_levels_modulator.html Insulin HYPERLINK https:/www.MedChemE/Insulin_levels_modulator.html HY

41、PERLINK https:/www.MedChemE/Insulin_levels_modulator.html levels HYPERLINK https:/www.MedChemE/Insulin_levels_modulator.html HYPERLINK https:/www.MedChemE/Insulin_levels_modulator.html modulatorCat. No.: HY-108719 Cat. No.: HY-112819Insulin glargine is a long-acting insulin analog.Insulin glargine c

42、an be used for the diabetesmellitus.Insulin levels modulator could be used to treatdiabetes.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Insulin_cattle_.html Insulin(cattle)(Insulin from bovine pancr

43、eas) Cat. No.: HY-P1156 HYPERLINK https:/www.MedChemE/Kaempferitrin.html Kaempferitrin(Lespedin; Lespenephryl) Cat. No.: HY-N0628Insulin cattle (Insulin from bovine pancreas) is atwo-chain polypeptide hormone produced in vivo inthe pancreatic cells. Insulin cattle has oftenbeen used as growth supple

44、ment in culturing cells.Kaempferitrin is a natural flavonoid, possessesantinociceptive, anti-inflammatory, anti-diabetic,antitumoral and chemopreventive effects, andactivates insulin signaling pathway.Purity: 98.60%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.94%

45、Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ku14r.html KU14R HYPERLINK https:/www.MedChemE/ku14r.html HYPERLINK https:/www.MedChemE/Linsitinib.html LinsitinibCat. No.: HY-15481(OSI-906) Cat. No.: HY-10191KU14R is a new I(3)-R antagonist, wh

46、ichselectively blocks the insulin secretory responseto imidazolines.Linsitinib (OSI-906) is a potent, selective andorally bioavailable dual inhibitor of the IGF-1receptor and insulin receptor (IR) with IC s of 3550and 75 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

47、 mgPurity: 99.88%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/linsitinib-d3.html Linsitinib-d3 HYPERLINK https:/www.MedChemE/linsitinib-d3.html HYPERLINK https:/www.MedChemE/mid-1.html MID-1(OSI-906-d3) Cat. No.: HY-10191SCat. No.: HY-115461Linsiti

48、nib-d3 (OSI-906-d3) is the deuteriumlabeled Linsitinib. Linsitinib (OSI-906) is apotent, selective and orally bioavailable dualinhibitor of the IGF-1 receptor and insulinreceptor (IR) with IC s of 35 and 75 nM,50respectively.MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin53-insulin receptor substrate

49、-1) interaction.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/MSDC_0160.html MSDC HYPERLI

50、NK https:/www.MedChemE/MSDC_0160.html HYPERLINK https:/www.MedChemE/MSDC_0160.html 0160(Mitoglitazone; CAY10415) Cat. No.: HY-100550 HYPERLINK https:/www.MedChemE/msdc-0602k.html MSDC-0602K(Azemiglitazone potassium) Cat. No.: HY-108022AMSDC 0160 (Mitoglitazone) is a mitochondrialtarget of thiazolidi

51、nediones (mTOT)-modulatinginsulin sensitizer and a modulator ofmitochondrial pyruvate carrier (MPC). MSDC0160 is a thiazolidinedione (TZD) withantidiabetic and neuroprotective activities.MSDC-0602K (Azemiglitazone potassium), aPPAR-sparing thiazolidinedione (Ps-TZD), binds toPPAR with the IC of 18.2

52、5 M. MSDC-0602K50modulates the mitochondrial pyruvate carrier(MPC).Purity: 99.40%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nt219.html NT219Cat. No.: HY-145935 HYPERLINK https

53、:/www.MedChemE/NVP-ADW742.html NVP-ADW742(ADW742; GSK 552602A; ADW) Cat. No.: HY-10252NT219 is a potent and dual inhibitor of insulinreceptor substrates 1/2 (IRS1/2) and STAT3. IRS1/2and STAT3 are major signaling junctions regulatedby various oncogenes. NT219 affects IRS1/2degradation and inhibits S

54、TAT3 phosphorylation.NVP-ADW742 (ADW742) is an orally active, selectiveIGF-1R tyrosine kinase inhibitor with an IC of500.17 M. NVP-ADW742 inhibits insulin receptor (InsR)with an IC of 2.8 M. NVP-ADW742 induces50pleiotropic antiproliferative/proapoptotic biologicsequelae in tumor cells.Purity: 98%Cli

55、nical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/NVP-AEW541.html NVP-AEW541(AEW541) Cat. No.: HY-50866 HYPERLINK https:/www.MedChemE/NVP-TAE-226.html NVP-TAE HYPERLINK htt

56、ps:/www.MedChemE/NVP-TAE-226.html HYPERLINK https:/www.MedChemE/NVP-TAE-226.html 226(TAE226) Cat. No.: HY-13203NVP-AEW541 (AEW541) is a potent inhibitor of IGF-1Rwith IC50 of 0.15 M, also inhibits InsR, with IC50of 0.14 M.NVP-TAE 226 (TAE226) is a potent andATP-competitive dual FAK and IGF-1R inhibi

57、tor withIC s of 5.5 nM and 140 nM, respectively. NVP-TAE50226 (TAE226) also effectively inhibits Pyk2 andinsulin receptor (InsR) with IC s of 3.5 nM and 4450nM, respectively.Purity: 98.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.92%Clinical D

58、ata: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/oi338.html OI338 HYPERLINK https:/www.MedChemE/oi338.html HYPERLINK https:/www.MedChemE/peonidin-3-o-glucoside-chloride.html Peonidin HYPERLINK https:/www.MedChemE/peonidin-3-o-glucoside-chloride.h

59、tml HYPERLINK https:/www.MedChemE/peonidin-3-o-glucoside-chloride.html 3-O-glucoside HYPERLINK https:/www.MedChemE/peonidin-3-o-glucoside-chloride.html HYPERLINK https:/www.MedChemE/peonidin-3-o-glucoside-chloride.html chlorideCat. No.: HY-142663 Cat. No.: HY-W040127OI338 is an orally available, ult

60、ralong-actinginsulin analogue.Peonidin 3-O-glucoside chloride, an anthocyanin,act as an insulin secretagogue. Peonidin3-O-glucoside chloride can increase glucose uptakein HepG2 cells. Peonidin 3-O-glucoside chloridehas the potential for type-2diabetes comorbidities research.Purity: 98%Clinical Data: