Alirocumab (REGN 727) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia[1].
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL)[1].
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
Rosuvastatin lactone is a metabolite of Rosuvastatin (HY-17504A) (HMG-CoA inhibitor)[1].
Hippuric acid-15N (2-Benzamidoacetic acid-15N) is the 15N-labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
ELX-02 disulfate (NB-124 disulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 disulfate is being developed as a therapy for genetic diseases caused by nonsense mutations[1].
Cysteamine is an agent for the treatment of nephropathic cystinosis and an antioxidant.Target: OthersCysteamine has been shown to increase intracellular glutathione levels in cystinotic cells, thus restoring the altered redox state of the cells. Also increased rates of apoptosis in cystinotic cells, which are thought to be the result of increased caspase 3 and protein kinase Cε activity, is counteracted by Cysteamine administration. Cysteamine has antioxidant properties as a result of increasing glutathione production. Cysteamine is an excellent scavenger of OH and HOCl; it also reacts with H2O2. Cysteamine increases the production of several heat shock proteins (HSP), including the murine Hsp40. Cysteamine exerts a dose-dependent effect on the doxorubicin-induced death of cancer cells, measured in both HeLa cells and B16 cells, whereas Cysteamine treatment alone had no influence on cell survival. In addition, in a doxorubicin-resistant breast cancer cell line, the addition of Cysteamine to doxorubicin results in a dramatic increase in cell death [1]. Cysteamine (100 μM) significantly is able to increase the intracellular GSH levels and the percentage of embryos that developed to the blastocyst stage of culture matured oocytes [2].
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS[1][2][3].
Omeprazole magnesium is an orally active proton pump inhibitor (PPI) and can suppress gastric acid. Omeprazole magnesium can be used for acid reflux-related symptoms and frequent heartburn research[1][2].
Thioacetamide-S-oxide, a Thiocetamide metabolite, is a δ-aminolevulinic acid (ALA) synthetase inhibitor[1].
Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH) is an adipokinetic hormone that regulates energy homeostasis in insects by mobilizing lipid and carbohydrate from the fat body. Adipokinetic hormone Gryllus bimaculatus stimulates the locomotor activity of the two-spotted cricket. Adipokinetic hormone Gryllus bimaculatus can also be used in studies to regulate body weight, induce weight loss and alleviate glycogen storage disorders in humans[1][2][3].
1alpha, 24, 25-Trihydroxy VD2 is a vitamin D analog.
2-Ethylpyrazine is an endogenous metabolite.
Endoglycoceramidase II (EGCase II) is an endo-β-glucosidase releasing the complete glycan from ceramide in glycosphingolipids. Endoglycoceramidase II Catalyzes the hydrolysis of the β-glycosidic linkage between oligosaccharides and ceramides in various glycosphingolipids[1][2].
DL-Mevalonolactone-d7 ((±)-Mevalonolactone-d7) is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
TA-1801 is a hypolipidemic agent.
Creatinine-D3 (NSC13123-D3) is a deuterium labeled Creatinine. Creatinine is a break-down product of creatine phosphate in muscle[1].
γ-Tocotrienol is an active form of vitamin E[1].
(Asp28)-Glucagon (1-29) (human, rat, porcine) is an optimized structure of glucagon, the 28th position is replaced by aspartic acid (Asp) which significantly increases the aqueous solubility of glucagon in a physiological pH buffer, has the same activity as glucagon[1].
SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM)[1][2].
Ficusonolide has significant antidiabetic activity with a possible mechanism of interaction with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.
Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.
Tetradecyl-β-D-maltoside is an absorption enhancer which can increase the nasal absorption of regular human insulin or the fast acting insulin analog lyspro-insulin[1].
KAT681 is a liver-selective thyromimetic.
Etidronic acid (Etidronate) disodium is an orally and intravenously active bisphosphonate. Etidronic acid disodium inhibits resorption of bone, reduces arterial calcification and can be used for osteoporosis research. Etidronic acid disodium has anticancer activity. Etidronic acid disodium is a chelating agent and can be used to remove heavy metal in water[1][2][3][4].
RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4SPA IC50 and RBP4–TTR FRET IC50 values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively[1].
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.