Endocrinology

Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.

Giripladib (PLA-695) is a selective cPLA_2α inhibitor. Giripladib attenuates CKD serum-induced PUFA accumulation, MDA and ROS levels, restores the GSH/GSSG ratio, and alleviates mitochondria-Ferroptosis-related morphological changes. Giripladib exhibits anti-inflammatory and disease-modifying effects in collagen-induced arthritis. Giripladib can be used in research on chronic kidney disease-associated plaque vulnerability, rheumatoid arthritis, and breast cancer.

Chlorpropamide is an oral hypoglycemic agent that can influence acetaldehyde metabolism in mice and has a potentiating effect on antidiuretic hormone.

CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC₅₀ of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive.

Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC₅₀ of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC₅₀s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.

Tetrahydroalstonine ((-)-Tetrahydroalstonine) is an indole alkaloid and a selective α₂-adrenergic receptor antagonist. Tetrahydroalstonine exhibits certain neuroprotective effects. Tetrahydroalstonine can regulate autophagy-lysosomal function by activating the Akt/mTOR pathway, significantly reducing OGD/R-induced primary cortical neuronal injury.

Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.

NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.

Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with K_is of 3.7 nM, 20 nM and 1.2 nM for the cloned human α_1a-, α_1b- and α_1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.

Aloin B (Isobarbaloin) is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC₅₀ of 16.08 μM (hydrolytic activity) and 17.51 μM (deubiquitinase activity). Aloin B is metabolized by rat intestinal flora into aloe-emodin-9-anthrone to exert laxative effects. Aloin B inhibits TPA (HY-18739)-induced ear edema, putrescine elevation, and tumor promotion in mouse skin. Aloin B can be used in research related to anti-inflammation, tumor promotion inhibition, coronavirus disease 2019 (COVID-19) and constipation.

Dexchlorpheniramine maleate is an orally taken anti-histamine that has anti-inflammatory, anti-irritant, anti-allergic, and skin barrier effects. Dexchlorpheniramine maleate inhibits myocardial contraction in rats. Dexchlorpheniramine maleate can be used in studies of allergic rhinitis.

Dihexyl phthalate is an orally active phthalate ester (PAEs) widely used as a plasticizer, and it acts as an environmental endocrine disruptor. Dihexyl phthalate exhibits endocrine-disrupting and reproductive toxic properties, induces oxidative stress and inflammation, and ultimately causes apoptosis and damage to reproductive organs such as the testes. Dihexyl phthalate can be used in studies related to developmental toxicity, embryonic lethality, teratogenicity, and abnormal development of the male reproductive system.

Labetalol hydrochloride (Standard) is the analytical standard of Labetalol hydrochloride (HY-B1108). This product is intended for research and analytical applications. Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.

GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β₂-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ₂-adrenoceptor with K_i values of 1.4, 1.3 and 3.7 nM, respectively.

Histamine (Standard) is the analytical standard of Histamine (HY-B1204). This product is intended for research and analytical applications. Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge.

3,4-Dihydroxyphenylglycol is a phenolic compound and antioxidant. 3,4-Dihydroxyphenylglycol can be extracted from olive oil. 3,4-Dihydroxyphenylglycol downregulates the expression of proinflammatory enzymes (iNOS, COX-2) and prevents the degradation of IκBα. 3,4-Dihydroxyphenylglycol has antioxidant properties. 3,4-Dihydroxyphenylglycol has shown positive effects on frozen-thawed ram sperm. 3,4-Dihydroxyphenylglycol can be used in the study of inflammatory-related diseases (such as ulcerative colitis) and reproductive health (sperm cryopreservation).

CL-387785 (EKI-785; WAY-EKI 785) is an orally active EGFR inhibitor with an IC₅₀ of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC₅₀ of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.