Diadenosine pentaphosphate pentasodium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes[1][2].
14-Deoxyandrographolide, a bioactive compound of Andrographis paniculata, has hepatoprotective efficacy. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release[1].
D-Glucosamine 6-phosphate is an endogenous metabolite that can be synthesized by glutamine fructose-6-phosphate amidotransferase (GFAT). D-Glucosamine 6-phosphate can be used for the research of diabetes mellitus[1].
Ethylmalonic acid is non-carcinogenic potentially toxic and associated with anorexia nervosa and malonyl-CoA decarboxylase deficiency.
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) 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[2][3].
DL-Alanine-1-13C is the 13C-labeled DL-Alanine. DL-alanine, an amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine, and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver[1][2][3][4][5][6].
LGD-6972 is a glucagon receptor antagonist.
Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects[1].
MC 976 is a Vitamin D3 derivative.
L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2[1].
Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of cocaine-seeking behavior in rats[1][2][3].
Hi 76-0079 (Compound 31) is a hormone-sensitive lipase (HSL) inhibitor with an IC50 of 184 nM[1].
MitoBloCK-10 (MB-10) is a potential attenuator of protein import into mitochondria via targeting Tim44, inhibits the import of substrates that use the TIM23 import pathway; targets Tim44 and mutations in the α4 helix of the C-terminal domain of Tim44 confer resistence to MitoBloCK-10 (MB-10); MitoBloCK-10 (MB-10) inhibits Tim44 binding to the precursor and to Hsp70, but not other component of the PAM complex; inhibits Hela cell viability with IC50 of 17.2 uM in MTT assays, impairs cardiac development and induces apoptosis in zebrafish.
Fructooligosaccharides (Oligolevulose) is a beneficial sugar which can be produced by the microbial flora. Fructooligosaccharides had no significant effect on blood glucose, blood lipid and serum acetate in diabetic model[1].
Sarmenoside III is a flavonol glycoside with hepatoprotective activity isolated from Sedum sarmentosum.
Celosin H is a hepatoprotective triterpenoid saponin that can be isolated from Celosiae Semen[1].
MitoEbselen-2, also known as MitoPeroxidase-2, is a radiation mitigator which reduces lipid hydroperoxides and prevents apoptotic cell death. When administered 24 hours postirradiation, MitoEbselen-2 was shown to increase the survival of mice exposed to whole body γ-irradiation.
all-trans-Anhydro Retinol (Anhydrovitamin A) is a metabolite of Vitamin A. all-trans-Anhydro Retinol is used in synthetic multivitamin preparations[1].
Bexagliflozin is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively.target: SGLT2IC50: 5.6 μM (SGLT1)/ 2 nM (SGLT2)1) In normal rats and dogs a saturable urinary glucose excretion was produced with an ED50 of 0.38 and 0.09 mg/kg, respectively.2) EGT1442 significantly prolonged the median survival of SHRSP rats.3) EGT1442 dose-dependently reduced HbA1c and blood glucose concentration without affecting body mass or insulin level.
Astin B is a orally active and potent cyclic pentapeptide, that can be isolated from Aster tataricus. Astin B has hepatotoxic effects in vitro and in vivo and that hepatic injury was primarily mediated by apoptosis in a mitochondria/caspase-dependent manner. Astin B induces autophagy in L-02 cells, increases LC3-II and decreases p62 expression[1].
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM[2]. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3].
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable drug-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model[1].
BCAT-IN-1 is a potent, selective and orally active inhibitor of BCATm, with a pIC50 of 7.3. BCAT-IN-1 shows 100-fold selectivity for BCATm over BCATc (pIC50=5.4). BCAT-IN-1 can be used for the research of metabolic diseases[1].
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].
Hylambatin, a tachykinin, increases both plasma glucose and plasma insulin, whereas the secretion of glucagon was not affected. Hylambatin can be used in diabetes research[1].
Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects.Target: Opioid ReceptorTrimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain [1]. The major product from drug metabolism of trimebutine in human beings is nor-trimebutine, which comes from removal of one of the methyl groups attached to nitrogen. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract [2, 3].
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases[1].
Pemvidutide is a GLP-1R/GCGR dual agonist, shows striking reductions in body weight, liver fat and serum lipids. Pemvidutide can be used in non-alcoholic steatohepatitis (NASH) and obesity research[1].
Meprednisone is a glucocorticoid and a methylated derivative of prednisone.Target: Glucocorticoid ReceptorMeprednisone is a glucocorticoid and a methylated derivative of prednisone. The methylprednisone to MPL area under the curve ratio decreased from 0.19 +/- 0.04 in control to 0.14 +/- 0.03 in ketoconazole-treated rats (P less than .05) due to altered interconversion between these steroids. An improved pharmacokinetic/dynamic receptor/gene-mediated model characterized the steroid receptor binding and induction of tyrosine aminotransferase activity after i.v. MPL sodium succinate (10 mg/kg). In contrast to previous in vitro studies, ketoconazole at maximally tolerated doses failed to antagonize the steroid receptor-mediated activity of MPL [1].