Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease[1][2][3].
Fmoc-Leu-Thr(psi(Me,Me)pro)-OH is a dipeptide.
4-Ethyl-2-methoxyphenol-d5 is the deuterium labeled 4-Ethyl-2-methoxyphenol[1].
IL-17 modulator 5 (compound 26) is a IL-17 inhibitor, with an IC50 of 1 nM[1].
Yadanziolide A, a quassinoid glycoside from Brucea javanica, has antitumor activity[1].
Dioleoylphosphatidylglycerol (DOPG) is a naturally occurring phospholipid that can be produced by the combined action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). Dioleoylphosphatidylglycerol inhibits macrophage inflammatory mediator production in response to heat shock protein B4 (HSPB4) activation of toll-like receptor 2 (TLR2) [1].
Bococizumab (PF-04950615) is an anti-human PCSK9 inhibitory antibody that reduces LDL cholesterol levels. Bococizumab can be used in the research of hypercholesterolemia[1][2].
Pseudocoptisine acetate, a quaternary alkaloid with a benzylisoquinoline skeleton, is isolated from the tubers of Corydalis turtschaninovii. Pseudocoptisine acetate shows anti-inflammatory properties[1].
Manwuweizic acid is a triterpenoid that can be isolated from Kadsura heteroclite[1].
Propylparaben is an antimicrobial agent, preservative, flavouring agent.
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis[1]. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors[2]. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor[3].
Chloro-PEG5-chloride is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
14:0-14:0 PC-d27 is deuterium labeled 14:0-14:0 PC.
Arvenin I is a natural cucurbitacin glucoside with moderate anticancer effects[1].
TLR7 agonist 10 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.Target: PDE5Udenafil is an oral PDE5 inhibitor. Udenafil significantly increased cAMP and cGMP levels and were more highly distributed in the prostate than plasma. The T/P ratio of udenafil was higher than tadalafil. These findings may help in the assessment of the feasibility of using PDE5 Is to concurrently treat both LUTS and erectile dysfunction [1]. After 12 weeks of treatment, the patients treated with udenafil showed significantly greater change from baseline in the IIEF-EF domain score compared with placebo (placebo, 0.20; 100-mg udenafil, 7.52; and 200-mg udenafil, 9.93, respectively) (P < 0.0001). udenafil significantly enhanced the rates of successful penetration (SEP Q2) and maintenance of erection (SEP Q3) (P < 0.0001) [2].
Adipokinetic Hormone (Apis mellifera ligustica, Bombyx mori, Heliothis zea, Manduca sexta) is a common peptide among various insects. Adipokinetic Hormone induces strong adipokinetic/hypertrehalosemic response. However Adipokinetic Hormone has no a glycogen-mobilizing function nor an adequate glycogen store in fat body for its effective utilization[1].
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction[1].
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
Quercetin-3-glucoside is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties.Quercetin-3-glucoside alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway[1].Quercetin-3-glucoside regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Quercetin-3-glucoside has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies[2].
Peonidin-3-O-arabinoside chloride (Compound Ⅻ) is an anthocyanin that can be isolated from Vaccinium myrtillus L.[1].
Oxantel (CP-14445), a m-oxyphenol derivative of Pyrantel (HY-12641), is a N-subtype AChR agonist. Oxantel is an anthelmintic, with excellent trichuricidal properties[1][2].
PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research[1].
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1].
NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner[1][2].
rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1 receptor antagonist. rel-O-2050 also decreases food intake in mice[1].
Piprofurol is a calcium channel inhibitor. Piprofurol inhibites in a concentration-dependent manner the calcium-induced contractions in isolated potassium depolarized preparations of rat aorta and relaxes the K+-induced contraction of the dog coronary artery and the rabbit basilar artery. Piprofurol exerts a negative inotropic effect on guinea-pig papillary muscle, with the EC50 of 5 μM[1].
Torsemide is a pyridine-sulfonyl urea type loop diuretic.Target: OthersTorasemide is a pyridine-sulfonylurea type loop diuretic mainly used in the management of edema associated with congestive heart failure. It is also used at low doses for the management of hypertension. Torsemide significantly reduced total HF readmissions (relative risk [RR]: 0.41, 95% CI: 0.28-0.61, p < 0.0001) and HF readmissions (RR: 0.53, 95% CI: 0.33-0.84, p = 0.008) as well as CV readmissions (RR: 0.77, 95% CI: 0.60-0.98, p = 0.03) in patients with "at least 1 readmission." Torsemide caused a 14% reduction in all-cause mortality (RR: 0.86 [0.53-1.39], p = 0.54). Torsemide significantly reduces HF and CV-related hospital readmissions in systolic HF. Furthermore, torsemide is associated with a trend in reducing all-cause mortality [1]. Torsemide has several characteristics that make it suitable for treatment of advanced heart failure including longer half-life, increased potency of diuretic action, and anti-aldosterone effects. This case report details the administration of torsemide in 3 dogs with advanced heart failure and apparent furosemide resistance [2].