type 1 diabetic

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

M617 acetate is a selective agonist of galanin receptor 1 (GAL1). M617 acetate acts through central GAL1, promotes GLUT4 expression, and enhances GLUT4 content in the cardiac muscle of type 2 diabetic rats. The Ki values are 0.23 and 5.71 nM for GAL1 and GAL2, respectively.

Semaglutide TFA is a glucagon-like peptide-1 congener that induces weight loss, lowers blood glucose levels, and reduces cardiovascular risk in diabetic patients.Semaglutide TFA induces mild-to-moderate and transient gastrointestinal disturbances, and may be used in the study of type 2 diabetes and obesity.

SKI2852 is an orally active, selective, and efficient 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, improving metabolic syndrome in diabetic mouse models.

MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transaminase (ALT), as well as serum and hepatic cholesterol and triglyceride, levels and reduces markers of NASH in the same model. |1. Bays, H.E., Schwartz, S., Littlejohn, T., 3rd, et al. MBX-8025, a novel peroxisome proliferator receptor-δ agonist: Lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J. Clin. Endocrinol. Metab. 96(9), 2889-2897 (2011).|2. Haczeyni, F., Wang, H., Barn, V., et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol. Commun. 1(7), 663-674 (2017).

1. Rhapontin (Ponticin) can alleviate liver steatosis and improve blood glucose and lipid profiles in KK Ay diabetic mice, indicates that rhaponticin has a noticeable antidiabetic effect and could be potentially used as a new agent to treat type 2 diabetes mellitus and its complications.

SIK1 activator 1 can enhances the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice. SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis.

Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. It impedes the conversion of angiotensin I to angiotensin II, thereby reducing total peripheral resistance and systemic blood pressure. Imidapril has research value in hypertension, type 1 diabetic nephropathy, and chronic heart failure.

Imidapril hydrochloride (Tanapril) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 2.6 nM, used for the treatment of hypertension.

LY3325656 is a GPR142 agonist suitable for clinical testing in human. LY3325656 demonstrated anti-diabetic benefits in pre-clinical studies and ADME PK properties suitable for human dosing. LY3325656 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

M617 TFA, a selective galanin receptor 1 (GAL1) agonist, exhibits dissociation constants (Kis) of 0.23 nM for GAL1 and 5.71 nM for GAL2. Through activation of GAL1, M617 TFA enhances GLUT4 expression and content in the cardiac muscle of type 2 diabetic rats [1] [2].

Vasonatrin Peptide (VNP) TFA, a chimeric compound derived from atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP), exhibits venodilating properties reminiscent of CNP, natriuretic effects akin to ANP, as well as unique arterial vasodilating capabilities not characteristic of either parent peptide. Additionally, VNP TFA confers cardioprotection in diabetic ischemia-reperfusion injury by attenuating endoplasmic reticulum (ER) stress through the cGMP-PKG signaling cascade [1] [2] [3].

GAD65 (524-543) is a biologically active peptide comprising amino acids 524 to 543 of glutamic acid decarboxylase 65 (GAD65). It represents an early islet antigen fragment that elicits proliferative T cell responses in the non-obese diabetic (NOD) mouse model, instrumental in spontaneous autoimmune diabetes research. The peptide serves as a specific, possibly low-affinity stimulant for the diabetogenic T cell clone BDC2.5. Notably, immunization with GAD65 (524-543) heightens NOD mice's vulnerability to type 1 diabetes when subjected to the adoptive transfer of BDC2.5 T cells.

CPL207280, an orally active GPR40 FFA1 agonist with antidiabetic effects, enhances glucose-stimulated insulin secretion and improves glucose tolerance in MIN6 pancreatic β-cells, healthy Wistar Han rats, and diabetic rat models, making it a valuable compound for type 2 diabetes research [1] [2].