Endocrinology/Hormones

GRT2932Q is a nonpeptidic agonist of the opioid receptor-like 1 (ORL1) [1].

<p>AR antagonist 6 (compound 6i), a diphenyl ether androgen receptor (AR) antagonist, binds to the AR with an affinity of 120 nM. It demonstrates low toxicity and effective in vitro activity in the golden Syrian hamster ear model. [19] [1]</p>

CGP-53153 is a steroidal inhibitor of 5 alpha-reductase (IC50s: 36 and 262 nM in rat and human prostatic tissue).

ASN04885796 is a neuroprotective, specific GPR17 agonist with an EC50=2.27 nM for GPR17-mediated GTPγS binding and study neurodegenerative diseases

L-6424 is an intermediate of Amiodarone and a non-selective ion channel blocker. It has an antiarrhythmic.

A 274 is a highly aromatic, monosubstituted phenol antioxidant generated during differentiation of neuroblastoma cells.

Estromustine, an active metabolite of estramustine phosphate, is used to treat prostate cancer.

GDC-2992 is a selective androgen receptor (AR) degradator that degrades AR and inhibits proliferation in VCaP cells,CRPC.

T3-ATA S-isomer, the S-isomer of T3-ATA, represents the active form of the thyroid hormone.

<p>Originally identified in Gila monster lizard (Heloderma suspectum), exendin-4 is an incretin mimetic, an analog of glucagon-like-peptide-1 (GLP-1), it stimulates insulin secretion and modulates gastric emptying to slow the entry of ingested sugars into the bloodstream. Exendin-4 is resistant to cleavage by plasma DPP-IV unlike GLP-1. This gives it a longer half-life and duration of action than GLP-1, as well as greater potency in vivo. Exendin-4 increases insulin sensitivity and improves glucose tolerance and is currently used for the treatment of Type 2 diabetes mellitus in its synthetic form Exenatide. Exendin-4 also promotes the production and proliferation of beta-cells leading to regeneration of the pancreas. It is a ligand to the exendin receptor and increases pancreatic acinni cAMP levels. However, the GLP-1 analog was found to have a toxic effect by inducing hypotension due to relaxation of the cardiac smooth muscle.</p>

L-Thyroxine-13C6 is the 13C labeled compound of L-Thyroxine. L-Thyroxine has a CAS number of 51-48-9. Levothyroxine is the major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.

Triamcinolone acetonide-d6 is a deuterated compound of Triamcinolone acetonide. Triamcinolone acetonide has a CAS number of 76-25-5. Triamcinolone acetonide is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Irbesartan-d4 (Irbesartan D4), a deuterated compound of Irbesartan, is an angiotensin receptor blocker and is used in the study of cardiovascular disease.

α-Cortolone, a metabolite of the glucocorticoid cortisol (hydrocortisone), is produced through the action of 20α-hydroxysteroid dehydrogenase (20α-HSD) via a tetrahydrocortisone (THE) intermediate. Studies indicate that urinary levels of α-cortolone are reduced in patients experiencing severe anorexia nervosa and postmenopausal women diagnosed with endometrial adenocarcinoma, in comparison to postmenopausal women without the condition.

Losartan D4 (DuP-753 D4) is a deuterated isotope of Losartan for isotopic tracing. Losartan is an angiotensin II receptor antagonist (IC50=20 nM).

<p>3,3',5-Triiodothyronine-(tyrosine ring-13C6) is the 13C labeled compound of 3,3',5-Triiodothyronine. 3,3',5-Triiodothyronine has a CAS number of 5817-39-0.</p>

VTP-27999 is an alkyl amine Renin inhibitor. VTP-27999 has been used in trials studying the basic science of Renal Function.

4-Hydroxytoremifene is a selective estrogen receptor modulator toremifene active metabolite.

UT receptor antagonist with pKB of 8.3; inhibits hU-II in aorta, no impact on other contractions/relaxations; partial agonist in Ca2+ assay.

Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride) , a tamoxifen metabolite, is effective specific Estrogen Response Modifier (SERM).