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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
7 Results for "
central active site
" in MedChemExpress (MCE) Product Catalog:
Products (7)
7 Results for "central active site" in MCE Product Catalog:
Synonyms: ZGN-1061
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Aclimostat (ZGN-1061) is a methionine aminopeptidase 2 (MetAP2) inhibitor. Aclimostat exhibits anti-obesity, anti-diabetic and ovarian cancer-related activities, and does not readily distribute to the central nervous system. Aclimostat acts on the active site of MetAP2 via irreversible covalent binding, and blocks enzyme activity through interactions with His231 and His339. Aclimostat regulates gene expression, reduces fat mass, plasma glucose, insulin levels, LDL-C, hs-CRP and leptin levels, while increasing adiponectin levels. Aclimostat can be used in research related to type 2 diabetes, overweight, obesity and ovarian cancer .
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UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB) .
Cat. No.: HY-107650
CAS No.: 139886-04-7
Synonyms: CI 979 hydrochloride; RU 35926 hydrochloride
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Milameline (CI 979; RU35926) hydrochloride is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydrochloride has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydrochloride has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline hydrochloride produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydrochloride can be used for the study of Alzheimer’s Disease .
Cat. No.: HY-135460
CAS No.: 139886-32-1
Synonyms: CI-979; RU35926
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Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease .
Cat. No.: HY-189042
CAS No.: 738562-57-7
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EF1500 is a potent human GABA transporter 1 (hGAT1) inhibitor and a lipophilic THPO analog. EF1500 occupies the binding site by forming a hydrogen bond with active residues of hGAT1 (such as Tyr139) through its exocyclic amino group, thereby blocking GABA reuptake. EF1500 can be used for research on central nervous system diseases .
Cat. No.: HY-107076
CAS No.: 554429-88-8
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Estrogen receptor modulator 14 is a chromene-derived prodrug of selective Estrogen Receptor modulator with oral activity. Estrogen receptor modulator 14 undergoes hydrolysis in vivo to produce the active metabolite 2d-(R), which acts on ERα and ERβ. Estrogen receptor modulator 14 acts on central thermoregulatory sites and possesses the ability to regulate estrogen signaling in multiple systemic tissues. Estrogen receptor modulator 14 maintains antiestrogenic activity in the uterus, and alters plasma cholesterol and bone metabolism. Estrogen receptor modulator 14 can be used for the research of estrogen receptor-related diseases .
Cat. No.: HY-107650A
Purity: 96.25%
Synonyms: CI 979 hydroiodide; RU 35926 hydroiodide
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Milameline (CI 979; RU35926) hydroiodide is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydroiodide has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydroiodide has a higher affinity for sites [ 3H]CMD (IC50 = 20 nM), than [ 3H]QNB, (IC50 = 3059 nM). Milameline hydroiodide produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydroiodide can be used for the study of Alzheimer’s Disease .
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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
