BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.
20-Carboxy-Leukotriene B4 (20-COOH LTB4) is a metabolite of Leukotriene B4 (LTB4; HY-107608). 20-Carboxy-Leukotriene B4 binds to the BLT1 receptor with high affinity. 20-Carboxy-Leukotriene B4 inhibits LTB4-mediated neutrophil responses (migration, degranulation, leukotriene biosynthesis)[1].
Forrestiacids J is an ATP-citrate lyase (ACL) inhibitor with an IC50 of 2.6 μM[1].
Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
(R)-Pyrrolidine-2-carboxylic acid-d3 ((+)-(R)-Proline-d3) is the deuterium labeled (R)-pyrrolidine-2-carboxylic acid. (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
Monoolein-d7 is deuterium labeled Monoolein. Monoolein is an endogenous metabolite.
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction[1].
NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
4-Hydroxy Atorvastatin lactone is a metabolite of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids[1].
L-Alanyl-L-leucine is an endogenous metabolite.
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
10-Formyl-7,8-dihydrofolic acid is a substrate for mammalian aminoimidazolecarboxamide ribotide transformylase (EC 2.1.2.3). 10-Formyl-7,8-dihydrofolic acid also is a metabolite of 10-HCO-H4folate[1][2].
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A[1].
β-Carotene-d10 (Provitamin A-d1) is the deuterium labeled β-Carotene. β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities[1][2][3][4][5].
SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. Glucosylsphingosine is a very promising, reliable and specific biomarker for monitoring Gaucher disease[1].
2,3,5-Trimethylpyrazine is an endogenous metabolite.
CDN1163 is a sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) activator.
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research[1].
Bentracimab (PB 2452) is a neutralizing monoclonal antibody that binds Ticagrelor (HY-1006) and its major active circulating metabolite with high affinity. Bentracimab can rapidly reverse the antiplatelet effect of Ticagrelor[1].
N1,N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively stabilizes SSAT enzyme activity[1].
Mannose 1-phosphate is an endogenous metabolite. Mannose 1-phosphate can be used to synthesize GDP-Man by the enzyme GDP-mannose pyrophosphorylase[1].
6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
Furosemide sodium (Lasix) is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.Target: NKCC Furosemide (INN/BAN) or frusemide is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi under the brand name Lasix, and also under the brand names Fusid and Frumex. It has also been used to prevent Thoroughbred and Standardbred race horses from bleeding through the nose during races.Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs.Furosemide, like other loop diuretics, acts by inhibiting NKCC2, the luminal Na-K-2Cl symporter in the thick ascending limb of the loop of Henle. The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone; it also abolishes the corticomedullary osmotic gradient and blocks negative, as well as positive, free water clearance.Because of the large NaCl absorptive capacity of the loop of Henle, diuresis is not limited by development of acidosis, as it is with the carbonic anhydrase inhibitors. Additionally, furosemide is a noncompetitive subtype-specific blocker of GABA-A receptors. Furosemide has been reported to reversibly antagonize GABA-evoked currents of α6β2γ2 receptors at ?M concentrations, but not α1β2γ2 receptors. During development, the α6β2γ2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide
NSC 8751-d6 is the deuterium labeled NSC 8751[1]. NSC 8751 is an endogenous metabolite[2].
Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice[1].
MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].
(R)-Aminocarnitine (Emeriamine) is a fatty acid oxidation inhibitor. (R)-Aminocarnitine reduces hyperglycaemia and ketosis. (R)-Aminocarnitine can be used in the study of metabolic diseases[1].