Boldenone undecylenate(Equipoise) is a synthetic steroid which has a similar effect as the natural steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans.IC50 Value: Target: The effects of this steroid are more subtle than that of many other steroids.in vitro: in vivo: Rabbits were injected intramuscularly twice weekly for two months. BOL had no significant effect on the bwt and bwt gain. Testes and epididymis weights were decreased significantly in the BOL-treated groups. BOL caused significant reduction in serum testosterone level, seminal volume, sperm motility, and sperm count [1].
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity[1][2].
NAPQI is the toxic metabolite of Paracetamol. NAPQI is also an inhibitor of enzymes in the vitamin K cycle. NAPQI is rapidly detoxified by glutathione (GSH), but in situations of GSH deficiency, excess NAPQI reacts with cysteine residues in proteins, causing cell death and toxicity in the liver[1][2].
KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
Tricaprin (Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA) and can be hydrolyzed to DA. Tricaprin (Glyceryl tridecanoate) is a major component of medium chain triglyceride (MCT) with antiandrogen and antihyperglycemic properties[1].Tricaprin (Glyceryl tridecanoate) has a safe use in in foods, drugs, cosmetics as an additive[2].
PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]
Trichlormethiazide is a thiazide diuretic with properties similar to those of hydrochlorothiazide.Target: OthersTrichlormethiazide is a diuretic with properties similar to those of hydrochlorothiazide. It is usually administered for the treatment of oedema (including that which is associated with heart failure, hepatic cirrhosis and corticosteroid therapy) and hypertension. In veterinary medicine, trichlormethiazide can be combined with dexamethasone to be used on horses with mild swelling of distal limbs and general bruising. Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle. This results in excretion of sodium, chloride and water, and thus acts as a diuretic [1-3].
AT-1002, a 6-mer synthetic peptide[1], is a tight junction regulator and absorption enhancer[2].
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice[1].
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders[1].
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].
Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM). Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2.
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
Interiotherin A is a lignan with a dibenzocyclooctadiene skeleton isolated from Kadsura interior. Interiotherin A inhibits HIV replication to exhibit anti-HIV activity, it has a role as a metabolite and an anti-HIV agent[1].
ATP-γ-S tetrasodium, an ATP analogue, is a P2Y11 receptor agonist. ATP-γ-S tetrasodium is active in ATP hydrolysis. ATP-γ-S tetrasodium is also an antioxidant and neuroprotectant[1][2].
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
Poliumoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 value of 4.6-25.7 μM.IC50 value: Target: Poliumoside exhibited greater inhibitory effects on rat lens aldose reductase with IC50 values of 0.85 μM, than those of the positive controls, 3,3-tetramethyleneglutaric acid (IC50=4.03 μM) and quercetin (IC50=7.2 μM).
Vanin-1-IN-1 is an inhibitor of vanin-1 enzyme which is a cell surface associated, giycosyiphosphatidyS inositol (GPi) anchored protein and plays an important role in metabolism and inflammation[1].
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron.
Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity[1].
1-Methyl-L-histidine is an objective indicator of meat ingestion and exogenous 3-methylhistidine (3MH) intake.
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit[1][2].
L-Ornithine-d6 hydrochloride is the deuterium labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
Galactose 1-phosphate-13C potassium is the 13C labeled Galactose 1-phosphate Potassium salt. Galactose 1-phosphate Potassium salt is is an intermediate in the galactose metabolism and nucleotide sug[1][2].
1-Deoxynojirimycin hydrochloride (Duvoglustat hydrochloride) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin hydrochloride suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin hydrochloride possesses antihyperglycemic, anti-obesity, and antiviral features[1][2].
GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
L-Arginine L-glutamate ((S)-(+)-Arginine L-glutamate) is the nitrogen donor for synthesis of nitric oxide. L-Arginine L-glutamate can be used for upper gastrointestinal hypofunction or dysfunction like functional dyspepsia research[1].
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase[1].
CAY10602 is a SIRT1 activator.