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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
293 Results for "
tissue selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (293)
293 Results for "tissue selectivity" in MCE Product Catalog:
28
28 Publications Verification
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CL316243 free acid is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors. CL316243 free acid is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 free acid has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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28 Publications Verification
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CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors .CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate . CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence .
21
21 Cited Publications
Synonyms: Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
Category:
Rutaceae Extract Plants Alkaloids Piperidine Alkaloids Phenols Polyphenols Disease Research Fields Endocrinology Tetradium ruticarpum (A. Jussieu) T. G. Hartley Cancer
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17
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Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action .
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Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action .
9
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice .
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8 Cited Publications
Synonyms: Poly-p-methoxyphenethylmethylamine
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Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
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8 Cited Publications
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IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
8
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Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
8
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Clorgyline (M&B 9302) is a selective, irreversible monoamine oxidase A (MAO-A) inhibitor that can cross the blood-brain barrier and exhibits activity against the 5-HT Receptor at very high doses. Clorgyline regulates monoamine neurotransmitter levels, the release of dopamine and acetylcholine, the uptake and effects of Tyramine (HY-W007606), noradrenergic function, circadian locomotor activity rhythms, feeding behavior, and body weight. Clorgyline induces tumor-suppressive transcriptional programs, secretory differentiation, androgen signaling regulation, Bcl-2 expression, and radioprotective effects in non-malignant cells. Clorgyline is used in the research of high-grade prostate cancer, Huntington's disease, major affective disorder, radiation-induced normal tissue toxicity, and obesity .
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8 Cited Publications
Synonyms: M&B 9302 hydrochloride
Clorgyline hydrochloride (M&B 9302 hydrochloride) is a selective, irreversible monoamine oxidase A (MAO-A) inhibitor that can cross the blood-brain barrier and exhibits activity against the 5-HT Receptor at very high doses. Clorgyline hydrochloride regulates monoamine neurotransmitter levels, the release of dopamine and acetylcholine, the uptake and effects of Tyramine (HY-W007606), noradrenergic function, circadian locomotor activity rhythms, feeding behavior, and body weight. Clorgyline hydrochloride induces tumor-suppressive transcriptional programs, secretory differentiation, androgen signaling regulation, Bcl-2 expression, and radioprotective effects in non-malignant cells. Clorgyline hydrochloride is used in the research of high-grade prostate cancer, Huntington's disease, major affective disorder, radiation-induced normal tissue toxicity, and obesity .
7
7 Cited Publications
Cat. No.: HY-18102
CAS No.: 1215085-92-9
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GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .
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7 Cited Publications
Synonyms: AT2 receptor agonist C21
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis .
7
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Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Category:
Natural Products Endogenous metabolite Disease Research Fields Inflammation/Immunology Endocrinology
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5 Cited Publications
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GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
5
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Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
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5 Cited Publications
BSJ-03-123 is a selective PROTAC degrader of CDK6. BSJ-03-123 degrades CDK6, thereby inhibiting Rb S780 phosphorylation and inducing G1 phase arrest, while remodeling cell cycle and transcriptional signaling, with no effect on CDK4-dependent cancer cells. BSJ-03-123 reduces CDK6 protein levels in mouse ovarian tissues, increases the proportion of primordial follicles, and induces granulosa cell apoptosis, without impairing the ability of oocytes to resume meiosis and mature to the MII stage. BSJ-03-123 alleviates uveitis by blocking the HDACs-CDK6/ID2 axis. BSJ-03-123 can be used in studies related to acute myeloid leukemia, mantle cell lymphoma and autoimmune uveitis .
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4 Cited Publications
Synonyms: MK-2866; GTX-024; Enobosarm
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Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism .
4
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GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
