OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesteronereceptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity.
ZK 216348 also binds to Progesterone and mineralocorticoid receptors (IC50s: 20.4 nM and 79.9 nM, respectively). ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist (IC50: 20.3 nM). ZK 216348 has an anti-inflammatory activity similar to
5β-Dihydroprogesterone (5β-DHP) is a progesteronereceptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesteronereceptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4
[Sar9]-Substance P is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.
Tebuconazole-d9 is intended for use as an internal standard for the quantification of tebuconazole by GC- or LC-MS. Tebuconazole is a triazole fungicide that is active against both seed and foliar fungi. It inhibits 14α-demethylase isolated from U. maydis and S. bicolor with IC50 values of 0.05 and 0.16 nM, respectively. It inhibits the androgenic effect of the androgen receptor agonist DHT (IC20 = 2.89 µM) and is cytotoxic (EC20 = 38.9 µM) in an MDA-kb2 assay. Tebuconazole (50 and 100 mg kg per day) administered during gestation reduces testosterone levels and increases testicular levels of progesterone and 17α-hydroxyprogesterone in male rat fetuses. It has a feminizing effect on male pups and a virializing effect on female pups. When administered to rats gestationally through postnatal day 42, tebuconazole (20 and 60 mg kg per day) leads to cell death of pyramidal cells in the CA3-4 region of the hippocampus and layer V of the cortex concomitant with impairment in learning......