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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
19 Results for "
Stereospecifically
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "Stereospecifically" in MCE Product Catalog:
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Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas .
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1 Cited Publications
ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors .
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SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM) .
Cat. No.: HY-W004114
CAS No.: 68-95-1
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Cat. No.: HY-W353804
CAS No.: 31501-19-6
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2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase .
Cat. No.: HY-W010554
CAS No.: 637-88-7
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1,4-Cyclohexanedione is a drug intermediate. 1,4-Cyclohexanedione is an accepted substrate of EryKR1 domain which takes on a certain biocatalyst activity and stereospecificity .
Cat. No.: HY-160431
CAS No.: 82864-43-5
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8(9)-EET is one of the main metabolites produced by the metabolism of arachidonic acid (HY-109590) through the cytochrome P450 epoxide pathway. 8(9)-EET is an effective substrate for COX-1 and COX-2. 8(9)-EET activates PPARα in HEK293 cells and inhibits the activity of NF-κB induced by IL-1β in a PPARα-dependent and -independent manner. The (8S,9R)-isomer of 8(9)-EET ([(8S,9R)-EET]) causes vasoconstriction, thereby reducing renal plasma flow and glomerular filtration rate .
Cat. No.: HY-118833
CAS No.: 25360-99-0
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RAC 109 is a local anesthetic. RAC 109 reduces ventricular conduction velocity and myocardial contractility in rabbits in a stereospecific manner (EC50=30 μM) .
Cat. No.: HY-W351380
CAS No.: 98674-83-0
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(-)-Anicyphos is a chiral catalyst with the activity of promoting the selectivity of specific reactions. (-)-Anicyphos is often used to synthesize complex chiral molecules in organic synthesis and shows excellent catalytic performance. By adjusting the reaction conditions, (-)-Anicyphos can significantly improve the stereospecificity of the product, providing an effective strategy for compound development.
Cat. No.: HY-120777
CAS No.: 1403602-92-5
GSK729 is a THPP inhibitor with the activity of inhibiting EchA6 and inhibiting Mycobacterium tuberculosis. GSK729 can selectively pull down EchA6 in a stereospecific manner, inhibit its activity, inhibit fatty acid synthesis of Mycobacterium tuberculosis, and has a bactericidal effect in a mouse chronic tuberculosis infection model.
Cat. No.: HY-116284A
CAS No.: 7000-27-3
Synonyms: Methyl β-D-glucoside hemihydrate
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Methyl β-D-glucopyranoside (Methyl β-D-glucoside) hemihydrate is a model glycosyl acceptor for enzymatic glycosylation reactions. Methyl β-D-glucopyranoside hemihydrate participates in glycoside synthesis and can react with acyl donors such as caffeic acid esters under the catalysis of specific enzymes (such as Lipozyme TL IM) to achieve acylation modification. Methyl β-D-glucopyranoside hemihydrate can be used in organic synthesis and biocatalysis research, especially the efficient enzymatic preparation of medicinal glycosides (such as Robustaside B (HY-N2720), 6-O-caffeoyl salidroside) .
Cat. No.: HY-P2854A
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L-Alanine Dehydrogenase, Bacillus subtilis (EC 1.4.1.1) is an A-stereospecific dehydrogenase that catalyzes the reversible deamination of L-alanine to pyruvate and ammonium.
Cat. No.: HY-N20657
CAS No.: 1644058-82-1
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Cat. No.: HY-182543
CAS No.: 148717-47-9
NPS-467 is a calcium-sensing receptor (CaR) activator and stereospecific agent with only its R-enantiomer active. NPS-467 increases the sensitivity of the CaR to activation by extracellular calcium. NPS-467 stimulates stanniocalcin (STC) secretion in trout and induces inhibition of gill calcium transport in trout. NPS-467 has no effect on serum calcitonin levels in trout .
Cat. No.: HY-170623
CAS No.: 152914-63-1
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1-Palmitoyl-2-stearoyl-3-butyryl-rac-glycerol is a triacylglycerol containing Palmitic acid (HY-N0830), Stearic acid (HY-B2219), and Butyric acid (HY-B0350) at the sn-1, sn-2, and sn-3 positions, respectively. It has been used to determine the stereospecificity and typoselectivity of lipases.1
Cat. No.: HY-180898
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AHL-7160 is a covalent DGKα inhibitor that possesses dual functions of enzyme activity inhibition (IC₅₀ ≈ 12 nM) and molecular gel-mediated degradation. AHL-7160 can rapidly recruit endogenous DGKα to the cell membrane (EC₅₀ = 39 nM), and this effect has isozyme selectivity. AHL-7160 can stereospecifically block phosphatidylcholine acid (PA) production mediated by DGKα (IC₅₀ = 340 nM). AHL-7160 enhances T cell activation and promotes anti-tumor immune responses. AHL-7160 can be used for research on immunotherapy .
Cat. No.: HY-W787758
CAS No.: 24102-11-2
Synonyms: 4-yn-VPA
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2-Propylpent-4-ynoic acid (4-yn-VPA) is a HDAC inhibitor (with an IC50 of 0.5 mM against human HDAC). 2-Propylpent-4-ynoic acid also induces P-glycoprotein function, and exhibits teratogenicity, fetal growth inhibition and neurotoxicity. 2-Propylpent-4-ynoic acid shows significant stereospecific teratogenic effects, with the S-enantiomer being more teratogenic than the R-enantiomer and other analogs. The neurotoxicity of 2-Propylpent-4-ynoic acid is independent of its stereochemical structure. 2-Propylpent-4-ynoic acid has been used in studies related to the pathogenesis of colon cancer and neural tube defects such as exencephaly .
Cat. No.: HY-L949
1279 compounds
Spirocyclic compounds, with rigid 3D structures, high Fsp³ and strong conformational restriction, are highly privileged scaffolds in small-molecule drug screening. They overcome drawbacks of planar aromatic compounds such as poor solubility, high off-target risks and weak druggability. Their orthogonal bicyclic geometry fits well into protein pockets, improving target affinity, subtype selectivity, metabolic stability and membrane permeability, making them ideal for hit identification against kinases, GPCRs, PPIs and other targets.
Spirocyclic scaffolds have been widely applied in oncology, antivirals, hypertension and CNS diseases, leading to many approved drugs and clinical candidates. SAR studies show that spiro-atom chirality, ring size and heteroatom substitution dominate bioactivity and selectivity, with the scaffold mainly serving as a conformational anchor. Azaspirocycles, spirooxindoles and spirosteranes target GPCRs, kinases, MDM2-p53 and PPIs. Approved drugs including irbesartan, spironolactone and rolapitant confirm their druggability, while revumenib and SAR405838 show promise against undruggable targets.
The MCE Spirocyclic Druglike Library contains over 1,000 diverse, stereospecific molecules selected by Lipinski’s rules. It covers privileged cores such as azaspirocycles, oxaspirocycles and spirooxindoles. These molecules bear rich chiral centers and distinct 3D orientations, reducing non-specific binding and enhancing screening efficiency. Featuring novel scaffolds, the library offers a highly innovative starting point for drug discovery.
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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
