Endocrinology/Hormones

<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>

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.

<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>

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

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.

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.

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

4'-Raloxifene-β-D-glucopyranoside is a metabolite of Raloxifene.

Cilazapril Monohydrate (Justor) is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.

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

JNJ-37654032: orally active, nonsteroidal SARM. Mixed AR agonist/antagonist. Selective for muscle, grows levator ani, max at 3mg/kg, ED(50) 0.8mg/kg.

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

Procymidone is a broad-spectrum fungicide that inhibits fungal glycerol triester synthesis, thereby disrupting hyphal growth. androgen receptor (AR) antagonist

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

Diisopropyl phthalate is widely used as an additive in plastics and consumer products in the chemical industries.

Timobesone is a topical corticosteroid.

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

<p>Originally identified in Heloderma horridum horridum (Mexican beaded lizard), exendin-3 is in the glucagon family. Exendin 3 stimulates vasoactive intestinal peptide (VIP) receptors in high concentrations. This leads to increased cAMP levels and amylase secretion in the pancreas. However, low exendin-3 exposure only increases cAMP levels. In applications, exendin-3 was found to induce hypotension by relaxation of cardiac, smooth muscle. Using a tag, exendin-3 is being investigated as a stable agonist for GLP1R to detect insulinomas, a pancreatic B cell-derived cancer with high GLP1R expression. Exendin 3 has also been used on mouse models to assess its effect on glucose-stimulated insulin secretion in glucagon receptor knockout (Gcgr-/-) backgrounds. Understanding the interplay between exendin 3 and metabolism could provide new insights into the obesity crisis.</p>

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

Tolrestat (AY-27773) is a potent inhibitor of aldose reductase (IC50 = 35 nM).