Endocrinology

PROTAC TSSK1 Degrader-2 is a cereblon-recruiting PROTAC degrader targeting TSSK1, with a DC₅₀ of 10.8 nM and an IC₅₀ of 56.8 nM against TSSK1. PROTAC TSSK1 Degrader-2 recruits the cereblon E3 ubiquitin ligase to induce proteasomal degradation of TSSK1. PROTAC TSSK1 Degrader-2 reduces the motility and in vitro fertilization capacity of mouse sperm. PROTAC TSSK1 Degrader-2 undergoes metabolic N-dealkylation and exhibits high efflux. PROTAC TSSK1 Degrader-2 can be used in studies related to male fertility.

Palopegteriparatide (Transcon PTH) is a prodrug of parathyroid hormone PTH 1-34, which can maintain normal and stable calcium concentrations without the need for calcium and active vitamin D replacement. Palopegteriparatide can be used in research on hypoparathyroidism.

Anti-aging agent 2 is an anti-aging agent. Anti-aging agent 2 attenuates senescence-associated secretory phenotype (SASP), alleviates cell cycle arrest, reduces the levels of senescence markers in renal tissues, and downregulates the expression of p21, p16 and p53 in the kidney. Anti-aging agent 2 improves renal function and alleviates renal fibrosis. Anti-aging agent 2 extends the lifespan of Caenorhabditis elegans. Anti-aging agent 2 can be used in the research of chronic kidney disease.

Segetalin C is a cyclic peptide that increases uterine weight in ovariectomized rats (2.5 mg/kg).

Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.

Radix euphorbiae ebracteolatae extract is an extract of Radix Euphorbiae Ebracteolatae that can regulate aquaporins.

2'-Deoxyadenosine monohydrate-2′-¹³C is the ¹³C labeled 2'-Deoxyadenosine monohydrate(HY-W011683). 2′-Deoxyadenosine monohydrate is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine monohydrate inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine monohydrate activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine monohydrate inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine monohydrate inhibits the growth of various cells. 2'-Deoxyadenosine monohydrate has an anticancer effect on colon cancer.

Drospirenone-d₄-1 is deuterium labeled Drospirenone.

Org-9935 is a selective inhibitor of PDE3 with an IC₅₀ of 50 nM. Org-9935 inhibits maturation of oocyte in naturally selected dominant follicle in rhesus macaques. Org-9935 can augment glucose-induced insulin release in isolated rat islets with an EC₅₀ of 20 μM.

L14-8 is a potent ferroptosis inducer. L14-8 promotes PLK1 degradation via ubiquitination, increasing TP53 phosphorylation to enhance SAT1 transcription, thereby triggering ferroptosis and cancer cell death. L14-8 can be used for the study of advanced prostate cancer.

Chlorotrianisene-d₉ is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.

Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties.

Maropitant-d₃ is the deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.

JNK3-IN-11 is a selective JNK3 inhibitor with an IC50 of 2.08 nM. JNK3-IN-11 binds to the JNK3 ATP-binding pocket, forming conserved hydrogen bonds with Met149 and a water-mediated hydrogen bond with Lys93. JNK3-IN-11 suppresses TGF-β1-induced c-Jun phosphorylation, reduces profibrotic markers COL1A1 and PAI-1, restores E-cadherin expression, and has protection against podocyte injure. JNK3-IN-11 can be used for the research of chronic kidney disease.

VUF11207 (Compound 29) TFA is a CXCR7 agonist (pK_i of 8.1) that induces recruitment of β-arrestin2 (pEC₅₀ of 8.8) and subsequent internalization (pEC₅₀ of 7.9) of CXCR7.

L-Lysine-¹³C (dihydrochloride) is the ¹³C-labeled L-Lysine dihydrochloride. L-lysine dihydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.

(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production.

Talsupram is a selective noradrenaline inhibitor that has a high affinity for the noradrenaline transporter. Talsupram exhibits anti-hyperalgesic effects. Talsupram can decrease ethanol intake to the levels prior to REM-induced deprivation in rat model.

Indacaterol acetate is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol acetate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol acetate can also be used in cardiovascular disease research.

Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. Granuliberin R is a dodecapeptide, can act on rat peritoneal mast cell to liberate granules and release histamine.