insulin-like

Insulin-like Growth Factor II (IGF-2), the primary somatomedin in human serum, exerts both permissive and direct influences on neurite outgrowth and significantly improves the survival of sympathetic and sensory neurons [1] [2].

IGF-I 30-41 acetate(82177-09-1 free base) (Insulin-like Growth Factor I (30-41) acetate) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I).

IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions).IGF-I (24-41) (TFA) is amino acids 24 to 41 fragment of Insulin-like Growth

IGF-I (30-41) (TFA) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I).

IGF-I (24-41) is a 24-41 amino acid fragment of Insulin-like Growth Factor I (IGF-I), which contributes to systemic GH activities and exhibits various properties such as anabolic, antioxidant, anti-inflammatory, and cytoprotective.

IGF-I (30-41) is a fragment of Insulin-like Growth Factor I (IGF-I) comprising amino acids 30 to 41.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Mazdutide acetate is a potent co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR), a gastrin-regulating hormone analog.Mazdutide acetate stimulates insulin secretion from mouse pancreatic islets, and can be used in studies of obesity and type 2 diabetes (T2D).

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

D-chiro-Inositol (D-(+)-CHIRO-INOSITOL) is an epimer of myo-inositol that is found in certain mammalian glycosylphosphatidylinositol protein anchors and inositol phosphoglycans possessing insulin-like bioactivity.

S961 TFA is A high affinity insulin receptor (IR) antagonist with IC50 for hir-a, hir-b and human insulin-like growth factor I receptor (higf-ir) at 0.048, 0.027 and 630 nM, respectively.

neurotensin-like peptide that modulate pancreatic insulin and glucagon secretion/effects

Pinoresinol ((+)-Pinoresinol) has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and to reduce oxidative stress preserving pial blood flow distribution; it may exert pharmacologically interesting effects via modulation of the insulin-like signalling pathway in C.elegans. Pinoresinol causes an upregulation of the CDK inhibitor p21(WAF1 Cip1) both at mRNA and protein levels, inhibits NF-kappaB and activating protein 1 (AP-1).

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.

BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

NBI-31772 hydrate is a powerful inhibitor of the interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). It acts as a nonpeptide ligand, effectively releasing bioactive IGF-I from the IGF-I/IGFBP-3 complex (Ki values for all six human subtypes range from 1-24 nM). This compound demonstrates significant anxiolytic and antidepressant-like effects [1] [2] [3].

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, acts as a partial agonist at sst 2 sst 5 receptors, with IC50 values of 0.26 nM and 6.92 nM, respectively. It effectively inhibits the release of growth hormone and the production of insulin-like growth factor-1 (IGF-1), and either inhibits adenylate cyclase activity or promotes extracellular acidification. Angiopeptin TFA shows promise for use in coronary atherosclerosis research [1] [2].

PF-06372222 is a small-molecule negative allosteric modulator of the glucagon receptor (GCGR). PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion.

GIP, rat TFA (glucose-dependent insulinotropic polypeptide), a 42-amino acid peptide secreted by K cells in the duodenum and jejunum, promotes insulin release from pancreatic beta cells, supports beta cell proliferation, and enhances their survival. This rat-origin bioactive peptide, along with GLP (gastric-like peptide), belongs to the intestinal insulinotropic hormone family and is implicated in lipid homeostasis and potentially in the pathogenesis of obesity. Recent research suggests GIP's multifaceted role in these metabolic processes.

S961 TFA is a highly selective and high-affinity antagonist of the insulin receptor (IR), demonstrating IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for the human insulin-like growth factor I receptor (HIGF-IR) in SPA assays [1].

Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide, a biotin-labeled variant of glucagon-like peptide-1-(7-36), is a gastrointestinal peptide known for its antidiabetogenic properties, including enhancing insulin secretion [1] [2].

ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.

H-1356 is an insulin-like growth factor 1(IGF-I) analog that inhibits autophosphorylation of IGF-I receptor.

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

NBI-31772 (NBI 31772) is the potent inhibitor of insulin-like growth factor-1 binding protein (IGFBP, Ki = 47 nM). NBI-31772 can be used in research on IGF-responsive diseases.

Saxagliptin (BMS-477118) is a selective, reversible DPP4 inhibitor with an IC50 of 26 nM.

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

Efpeglenatide is a long-acting agonist of the glucagon-like peptide (GLP-1) receptor. efpeglenatide improves insulin sensitivity and slows weight loss in mice models of diabetes and obesity. efpeglenatide has been used in studies of type II diabetes.

13-POHSA (palmitoleic acid esterified to 13-hydroxy stearic acid) is a type of branched fatty acid esters of hydroxy fatty acids (FAHFAs), which have recently been discovered as endogenous lipids whose levels are modulated by fasting and high-fat diets, and are linked to insulin sensitivity in mice. Notably, the concentration of 13-POHSA in the serum significantly increases in glucose tolerant AG4OX mice, a model that overexpresses the Glut4 glucose transporter in adipose tissue, suggesting its physiological relevance. Like other FAHFAs, 13-POHSA is believed to enhance glucose tolerance, promote insulin secretion, and exert anti-inflammatory properties, highlighting its potential importance in managing metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs), endogenous lipids influenced by fasting and high-fat diets, are linked to improved insulin sensitivity in mice. These molecules consist of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) bonded to a C-16 or C-18 hydroxy fatty acid. A specific FAHFA, 5-POHSA, features palmitoleic acid esterified with hydroxy stearic acid at the 5th carbon. Elevated levels of 5-POHSA in the serum of AG4OX mice, which express high levels of the Glut4 glucose transporter in adipose tissue, correlate with glucose tolerance. Like other FAHFAs that enhance glucose tolerance, stimulate insulin secretion, and exhibit anti-inflammatory properties, 5-POHSA may play a role in managing metabolic syndrome and inflammation.

S961 is a high-affinity, selective insulin receptor (IR) antagonist with IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for human insulin-like growth factor I receptor (HIGF-IR) in scintillation proximity assays.

NVP-DPP728 is a potent, reversible, nitrile-dependent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an inhibition constant (K i) of 11 nM for human DPP-IV amidolytic activity. By inhibiting the degradation of glucagon-like peptide-1 (GLP-1), NVP-DPP728 enhances insulin release following glucose intake, making it useful for diabetes research [1].

Veligrotug is a chimeric monoclonal antibody of the IgG1-kappa class that targets the insulin-like growth factor 1 receptor (IGF1R, CD221) [1].

Cimdelirsen is a novel, ligand-conjugated, hepatic-targeted investigative antisense oligonucleotide designed to reduce growth hormone receptor (GHr) synthesis, thereby inhibiting the harmful effects of growth hormone (GH) hypersecretion and lowering circulating insulin-like growth factor-1 (IGF-1) levels in acromegaly patients.

(Ser8)-GLP-1 (7-36) amide, human, is a glucagon-like peptide-1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. This entero-insulinotropic hormone promotes glucose-dependent insulin secretion from pancreatic β-cells and affects gastrointestinal motility and secretion [1].

Robatumumab (Sch 717454), an anti-human insulin-like growth factor receptor-1 (IGF-1R) antibody, exhibits anti-tumor and anti-proliferative effects on cancer cells. It is applicable in research concerning osteosarcoma and Ewing sarcoma [1] [2].

S961 acetate is a selective and high-affinity antagonist of the insulin receptor (IR), demonstrating IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for the human insulin-like growth factor I receptor (HIGF-IR) in SPA assays [1].

D-Pinitol (Methylinositol) has anti-inflammatory activity. D-Pinitol(Methylinositol) exerts insulin-like activity, used for many diabetic associated conditions. D-Pinitol(Methylinositol) is a safe nutrient to reduce calorie consumption when supplementing with creatine.

Trofinetide, derived from the neuroprotective tripeptide Gly-Pro-Glu (an N-terminal sequence of insulin-like growth factor-1, IGF-1), shows promise in various neuroprotective models. At a concentration of 10 nM, it mitigates cell death in primary rat embryonic striatal neurons caused by okadaic acid. Additionally, Trofinetide reduces the expression of pro-inflammatory markers (IL-1β, TNF-α, IL-6, and E-selectin) in a rat model simulating neuroinflammation from penetrating ballistic-like brain injuries. In cases of brain injury induced by middle cerebral artery occlusion (MCAO), administration of Trofinetide at 30 and 60 mg/kg reduces the area of cortical and striatal infarct. Furthermore, a daily dose of 100 mg/kg reverses social recognition and contextual fear conditioning deficits, diminishes the number of dendritic spines, and decreases testicular weight gain in an fmr1-/- knockout mouse model of fragile X syndrome. Trofinetide formulations have been employed in treating Rett syndrome, highlighting its versatility across various neurological conditions.

AZ12253801 is a type 1 insulin-like growth factor receptor (IGF-1R) inhibitor.

Teneligliptin (MP-513) is a potent prolylthiazolidine-based DPP-4 inhibitor that competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

GKA50 quarterhydrate is a potent glucokinase activator with an EC50 value of 33 nM. This glucose-like activator of β-cell metabolism in rodent and human pancreatic islets is a Ca2+-dependent regulator of insulin secretion. It stimulates insulin secretion in mouse islets and significantly reduces blood glucose in high-fat-fed female rats.

Ganitumab (AMG 479) is a highly potent monoclonal antibody targeting the type 1 insulin-like growth factor receptor (IGF1R). Recognized for binding IGF1R at low concentrations with a KD value of 0.22 nM, Ganitumab inhibits IGF1R interactions with IGF1 and IGF2 in mice, making it useful for cancer research.

Figitumumab (CP-751871) is a fully human monoclonal antibody that targets the insulin-like growth factor 1 receptor (IGF1R) with high potency, achieving an IC50 value of 1.8 nM by inhibiting IGF1 binding to IGF1R, effectively blocking its activation [1].

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

Mecasermin (Human IGF-I; FK 780), a recombinant form of human insulin-like growth factor I (IGF-I), is promising for investigating growth failure attributed to growth hormone (GH) insensitivity due to defects in GH receptors or the presence of GH-inhibiting antibodies [1].

IGF-I (30-41) (TFA) is a fragment of Insulin-like Growth Factor I (IGF-I), comprising amino acids 30 to 41, that plays a role in systemic GH (Growth Hormone) activities and exhibits anabolic, antioxidant, anti-inflammatory, and cytoprotective properties [1].

10-OAHSA is a newly discovered endogenous lipid categorized within the group of branched fatty acid esters of hydroxy fatty acids (FAHFAs). This specific FAHFA comprises oleic acid esterified to 10-hydroxy stearic acid. It stands out among its FAHFA counterparts for its potential bioactive properties, similar to other members of its family such as PAHSAs, which are notably prevalent in the adipose tissue of AG4OX mice exhibiting glucose tolerance due to overexpression of the Glut4 glucose transporter specifically in adipose tissue. Like other FAHFAs, 10-OAHSA may play significant roles in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, which suggests its importance in managing metabolic syndrome and inflammation.