st-16

ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement

5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg kg) decreases immobility time in the forced swim test in mice. It increases time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at doses ranging from 30 to 50 mg kg. 5α-Androst-16-en-3α-ol protects against seizures induced by pentylenetetrazole or electroshock in mice (ED50s = 48.9 and 21.9 mg kg, respectively). 1.Brooksbank, B.W., Brown, R., and Gustafsson, J.A.The detection of 5α-androst-16-en-3α-ol in human male axillary sweatExperientia30(8)864-865(1974) 2.Kaminski, R.M., Marini, H., Ortinski, P.I., et al.The pheromone androstenol (5α-androst-16-en-3α-ol) is a neurosteroid positive modulator of GABAA receptorsJ. Pharmacol. Exp. Ther.317(2)694-703(2006)

5α-Androst-16-en-3-one, a mammalian pheromone present in boar saliva, plays a crucial role in facilitating social and sexual interactions by acting as a volatile chemical cue. It is utilized to prime sows in estrus for mating or artificial insemination, underscoring its significance in reproductive behavior. Additionally, this compound is detected in human sweat and urine, where it is involved in studies concerning receptor-mediated odorant detection and the genetic foundations of anosmias, thereby broadening its scope of relevance beyond the animal kingdom.

ST166 free acid 是一种抑制 PhoP-DNA 复合物形成的化合物，其IC50 值分别为 18 μM 和 24 μM，能够干扰 PhoP 和 MtrAC 与 DNA 的结合。此外，ST166 free acid 对海洋分枝杆菌展现出抑菌活性。

PPARγ agonist16 (Compound 4G) 是一种PPARγ激动剂，能够竞争性结合PPARγ的LBD结构域，其IC50为1790 nM。此化合物在小鼠模型中抑制耳朵肿胀，并在Streptozotocin诱导的小鼠糖尿病模型中展现抗高血糖作用。

GLP-1R agonist 16 (Compound 115a) 是一种GLP-1受体激动剂，EC50为 0.15 nM。

TLR7 agonist16 (compound 16d)为一种高效的TLR7激动剂，具有EC50值为59 nM。在低纳摩尔水平上，它可以有效激活小鼠巨噬细胞和hPBMC。

GLP-1 receptoragonist 16 (Example 53) 是一种GLP-1激动剂，用于研究糖尿病、肥胖及非酒精性脂肪性肝炎相关疾病。