Endocrinology

Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.

3,5-Dinitrocatechol (OR-486) is an orally active, blood-brain barrier-permeable selective catechol-O-methyltransferase (COMT) inhibitor. 3,5-Dinitrocatechol can be used in research related to Parkinson's disease, pheochromocytoma and adult cataract.

Taprenepag isopropyl is a highly selective EP₂ receptor agonist.

JNJ-5207852 is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1.

Meptyldinocap (2,4-DNOPC) is a fungicide and cytotoxic agent that acts against powdery mildew. Meptyldinocap upregulates the phosphorylation levels of ERK1/2, JNK and p38. Meptyldinocap induces apoptosis and endoplasmic reticulum stress, disrupts calcium homeostasis, inhibits cell proliferation and migration, downregulates the expression of proliferation- and pregnancy-related genes, and triggers mitochondrial dysfunction. Meptyldinocap can be used in studies related to powdery mildew and implantation failure.

GSK1059865 is a potent orexin 1 receptor antagonist.

γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na⁺) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R).

Lilial is a widely used synthetic fragrance and ester in consumer products. Lilial possesses estrogenic activity in vitro. Lilial can induce a toxic effect on mitochondria that causes a decrease in the viability of HaCaT cells. Lilial can increase NRF2 protein level in vitro. Lilial is able to target respiratory chain complexes, inhibit complexes I and II of the electron transport chain, increase the generation of reactive oxygen species, and decrease the level of intracellular ATP. Lilial can induce systemic toxicity in vivo. Lilial induces significant DNA strand breaks.

Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC₅₀s of 1.3 nM, 7.3 nM and K_is of 1 and 3 nM, respectively.

Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury.

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [¹²⁵I]-TARC to human CCR4 with a pIC₅₀ of 7.96.

Sevelamer carbonate is an orally active polymeric phosphate binder and bile acid sequestrant. Sevelamer carbonate binds dietary phosphate in the gastrointestinal tract, reducing phosphate absorption and serum phosphorus levels, and reduces urinary phosphate excretion. Sevelamer carbonate binds polyanion bile acids, increases bile acid faecal excretion, and reduces total cholesterol and LDL cholesterol levels. Sevelamer carbonate can be used for the research of hyperphosphataemia, hyperparathyroidism, chronic renal failure, kidney disease, and type 2 diabetes.

d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a K_i of 1.2 nM for human V1b receptor. d[Cha4]-AVP shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors.

Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H₃-receptor, with an IC₅₀ of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.

Gastrin I (1-14), human TFA is 1-14 fragment of human gastrin I peptide. Gastrin I is an endogenous, gastrointestinal peptide hormone. Gastrin is the major hormonal regulator of gastric acid secretion.

TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC₅₀s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC₅₀s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC₉₀s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.

Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, K_i is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats.

[Sar9,Met(O2)11]-Substance P is a tachykinin NK₁ receptor selective agonist.