Steroids

24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.

2-Hydroxyestradiol, a metabolite of 17β-estradiol with minimal estrogenic activity, possesses antioxidant effects and reacts with DNA to form stable adducts and exerts genotoxicity.

Cortisone acetate (Cortisone 21-acetate), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acetate acts as an immunosuppressant and anti-inflammatory agent. Cortisone acetate can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.

Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.

Estradiol valerate (β-Estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.

DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects and can be used for the research of cholesterol homeostasis diabetes.

Gracillin is a steroidal saponin that can be extracted from the roots of the plant and has anti-tumor properties. Gracillin can induce cancer cell apoptosis and autophagy.

Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 1 μM, 200-fold preference over TCPTP (IC₅₀ of 224 μM).

Cyproterone acetate is an anti-androgen (IC₅₀=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.

Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma.

Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC₅₀s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC).

Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway. Ruscogenin exerts significant anti-inflammatory and anti-thrombotic activities. Ruscogenin has orally bioactivity.

20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis.

Lathosterol is a plant sterol and cholesterol-like molecule. Lathosterol increases antioxidant enzymes (such as SOD, CAT, and GSH) and decreases LDH. Lathosterol has a hepatoprotective effect on mice with acetaminophen (HY-66005)-induced liver injury^[1].

Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice.

Fludrocortisone (9α-Fludrocortisone) is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.

Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.

Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABA_A receptor than its enantiomer form.

Digoxigenin (DIG) is a steroid. DIG is used for situ hybridization as a labeling molecule probe due to long shelf life and fast detection and high sensitivity of DIG-labeled riboprobes.