Caspase-3-IN-1 (compound 11b) is a potent Caspase-3 inhibitor, with an IC50 of 14.5 nM[1].
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM)[1].
Colestilan (MCI-196) is a non-absorbed, non-calcium-based phosphate binder and is also a non-metallic, anion exchange resin. Colestilan is orally active and can be used for hypercholesterolaemia research[1][2].
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice[1].
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models[1].
4,4'-Dimethoxychalcone, isolated from the plant Angelica keiskei koidzumi, acts as a natural autophagy inducer with anti-ageing properties[1].
MitoBloCK-6 is a potent Erv1/ALR inhibitor, with an IC50 of 900 nM and 700 nM, respectively. MitoBloCK-6 also inhibits Erv2 (IC50=1.4 μM). MitoBloCK-6 can induce apoptosis via cytochrome c release in hESCs[1].
BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice[1].
Allantoxanamide is a uricase inhibitor. Allantoxanamide-induced rats serve as animal models for studying purine biosynthesis, drug-induced hyperuricemia and hyperuricosuria, and related nephropathy[1].
3'-Hydroxy Repaglinide D5 is the deuterium labeled 3'-Hydroxy Repaglinide. 3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide[1].
α-D-Glucose-1-phosphate disodium hydrate is used as a starting material for synthesis of glucuronic acid. α-D-Glucose-1-phosphate disodium hydrate can be used as a cytostatic compound essential for cardiopathic therapy, as an antibiotic, as an immunosuppressive drug, and as a circulatory system therapy element[1].
Saikosaponin B4 is a member of saikosaponins isolated from the roots of B. falcatum, selectively inhibits ACTH-induced lipolysis[1].
Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout[1].
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
NHE3-IN-2 is a Na+/H+ exchanger-3 (NHE3) inhibitor ( patent WO2001079186A1, example 6-Chlor-4-phenyl-2-chinazolinyl-guanidin)[1].
Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ)[1].
Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
FOXO1-IN-3 is a highly-selective and orally active FOXO1 inhibitor. FOXO1-IN-3 reduces hepatic glucose production in mice. FOXO1-IN-3 improves insulin sensitivity and glucose control in db/db mice without causing weight gain[1].
Inonotusol F is a triterpene isolated from Inonotus obliquus. Inonotusol F shows hepatoprotective effects against D-galactosamine-induced WB-F344 cell damage[1].
Febuxostat acyl glucuronide (Febuxostat acyl-β-D-glucuronide) is a metabolite of Febuxostat (HY-14268). Febuxostat is a potent, selective and non-purine xanthine oxidase (XO) inhibitor[1].
TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2].
N-Oleoyl-L-Serine is an endogenous amide of long-chain fatty acids with ethanolamine (N-acyl amides). N-Oleoyl-L-Serine is a lipid regulator of bone remodeling and stimulates osteoclast apoptosis. N-Oleoyl-L-Serine can be used for antiosteoporotic drug discovery development[1].
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].
Vitamin B12 is a water soluble vitamin with a key role in the normal functioning of the brain and nervous system, and for the formation of blood.Target: OthersVitamin B12 is a water-soluble vitamin with a key role in the normal functioning of the brain and nervous system, and for the formation of blood. It is one of the eight B vitamins. It is normally involved in the metabolism of every cell of the human body, especially affecting DNA synthesis and regulation, but also fatty acid synthesis (especially odd chain fatty acids) and energy production. Vitamin B12 normally plays a significant role in the metabolism of every cell of the body, especially affecting the DNA synthesis and regulation but also fatty acid synthesis and energy production. However, many (though not all) of the effects of functions of B12 can be replaced by sufficient quantities of folic acid (vitamin B9), since B12 is used to regenerate folate in the body. Most vitamin B12 deficiency symptoms are actually folate deficiency symptoms, since they include all the effects of pernicious anemia and megaloblastosis, which are due to poor synthesis of DNA when the body does not have a proper supply of folic acid for the production of thymine due to methyl trapping. When sufficient folic acid is available, all known B12 related deficiency syndromes normalize, save those narrowly connected with the vitamin B12-dependent enzymes Methylmalonyl Coenzyme A mutase, and 5-methyltetrahydrofolate-homocysteine methyltransferase (MTR), also known as methionine synthase; and the buildup of their respective substrates (methylmalonic acid, MMA) and homocysteine.Coenzyme B12's reactive C-Co bond participates in three main types of enzyme-catalyzed reactions [1, 2].
Isoastragaloside I is a natural compound from the medicinal herb Radix Astragali; possesses the activity of elevating adiponectin production.IC50 value:Target:Astragaloside II and isoastragaloside I selectively increased adiponectin secretion in primary adipocytes without any obvious effects on a panel of other adipokines. Furthermore, an additive effect on induction of adiponectin production was observed between these two compounds and rosiglitazone, a thiazolidinedione class of insulin-sensitizing drugs. Chronic administration of astragaloside II and isoastragaloside I in both dietary and genetic obese mice significantly elevated serum levels of total adiponectin and selectively increased the composition of its high molecular weight oligomeric complex.
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β[1].
N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC50 and Ki of 3.76 and 2.34 μM, respectively.
Elcatonin (Carbocalcitonin) is a synthetic analog of eel calcitonin. Elcatonin increases bone mineral density, inhibits bone resorption and processes a central analgesic effect[1].
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
A selective inhibitor of the gelatinases MMP2 and MMP9 and MMP13 with Ki of 85, 150 and 120 nM, respectively; has minimal effect on other MMPs; accelerates diabetic wound healing by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound, thereby reversing the pathological condition.