Isotope-Labeled Steroids

Cholesterol-¹³C₅ is the ¹³C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.

Medroxyprogesterone acetate-d₃ is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.

Estrone-d₂ is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.

16α-Hydroxydehydroepiandrosterone-d₅ (16α-Hydroxy-DHEA-d₅) is the deuterium labeled 16α-Hydroxydehydroepiandrosterone (HY-113031).

Dexamethasone-d₃-1 (Hexadecadrol-d₃-1; Prednisolone F-d₃-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.

Methylprednisolone-d₂ is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.

Estrone-d₂-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.

Hydrocortisone-d₃ is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.

Cortodoxone-d₅ is the deuterium labeled Cortodoxone.

Cortodoxone-d₂ is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone).

Tetrahydrocortisol-d₅ is the deuterium labeled Tetrahydrocortisol. Tetrahydrocortisol is a metabolite of Hydrocortisone (HY-N0583) that fails to activate glucocorticoid receptor. Tetrahydrocortisol inhibits Dexamethasone (HY-14648)-induced formation of cross-linked actin networks. Tetrahydrocortisol acts as a synergist to enhance the activity of anticancer agents. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, ocular hypertension, lung cancer and breast cancer.

Prednisone-d₈ is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.

Spironolactone-d₇ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes.

Estriol-d₂ is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

Pregnenolone-d₄ is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

Ergosterol-d₃ is the deuterium labeled Ergosterol (HY-N0181). Ergosterol is the primary sterol found in fungi, with antioxidative, anti-proliferative, and anti-inflammatory effects.

27-Hydroxy cholesterol-d₆ is deuterium labeled 27-Hydroxy cholesterol.

7α-Hydroxycholesterol-d₇ is the deuterium labeled 7α-Hydroxycholesterol. 7α-Hydroxycholesterol is a cholesterol oxide and is formed by both enzymatic and non-enzymatic oxidation. 7α-Hydroxycholesterol can be used as a biomarker for lipid peroxidation.

21-Deoxycortisol-d₈ is the d₈-labeled 21-Deoxycortisol (HY-113405). 21-Deoxycortisol is an adrenal-specific C21 steroid that accumulates via alternative pathways due to 21-hydroxylase (CYP21A2/P450c21) deficiency. 21-Deoxycortisol serves as a sensitive and specific biomarker for steroid 21-hydroxylase deficiency (21OHD).

Tetrahydrocorticosterone-d₅ is the d₅-labeled Tetrahydrocorticosterone (HY-113422). Tetrahydrocorticosterone is a glucocorticoid. One of its active forms, 5α-Tetrahydrocorticosterone (HY-113364), exerts its effects by binding to the GC receptor and inhibiting inflammatory processes. Tetrahydrocorticosterone is naturally synthesized by the adrenal glands and plays a key role in regulating the metabolism of carbohydrates, proteins and fats.