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].
Beacon (47-73) is a C-terminal peptide fragment 47-73 of Beacon, and Beacon is a protein of 73 amino acid. Beacon (47-73) can be used for metabolic syndrome research[1][2].
Hi 76-0079 (Compound 31) is a hormone-sensitive lipase (HSL) inhibitor with an IC50 of 184 nM[1].
Gliquidone (AR-DF 26) is an anti-diabetic drug in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Loperamide D6 hydrochloride (R-18553 D6 hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
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.
TMPD dihydrochloride, a readily oxidizable compound, is an enzymatically convert redox active substrate molecule. TMPD dihydrochloride is also an electron donor and serves as a reducing cosubstrate for heme peroxidases[1][2]. TMPD dihydrochloride is also a complex IV substrate[3].
Pancreastatin (33-49), porcine is a pancreastatin fragment. Pancreastatin is a peptide isolated from porcine pancreas which has insulin-suppressive actions in vitro. Pancreastatin (33-49), porcine enhances the priming effect of glucose[1][2].
AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2].
URAT1 inhibitor 5 (compound 16) is a potent URAT1 inhibitor. URAT1 inhibitor 5 can be used in research of hyperuricemia[1].
Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone strength and bone mass; suppresses osteoclastic bone resorption in vivo.
(Rac)-Mirabegron D5 ((Rac)-YM178 D5) is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
NMTCA (NMTPRO) is a sulfur-containing N-nitrosamino acid. NMTCA can be used as an indicator of endogenous nitrosation by gas chromatography-thermalenergyanalysis[1][2].
XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis[1].
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].
Nequinate, a quinoline compound, is an anticoccidial agent against cecal coccidiosis (Eimeria tenella) infections[1]. Nequinate inhibits xanthine oxidoreductase (XOD) activity[2].
Evinacumab (REGN1500) is a humanised anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia[1].
Glyhexamide is an effective hypoglycemic agent in adult diabetics.
Sarmenoside III is a flavonol glycoside with hepatoprotective activity isolated from Sedum sarmentosum.
PROTAC PTPN2 degrader-1 (compound example 77) is a potent PTPN2 degrader. PROTAC PTPN2 degrader-1 has the potential for the research of cancer or metabolic disease[1].
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.
Segetalin B, a cyclopentapeptide from Vaccaria segetalis, possesses estrogen-like activity[1][2].
Palmitelaidic acid is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue.
2,8-Dihydroxyadenine, an endogenous metabolite, can cause the formation of urinary crystals and kidney stones. 2,8-Dihydroxyadenine can be used to diagnose adenine phosphoribosyltransferase (APRT) deficiency[1][2].