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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
202 Results for "
binding properties
" in MedChemExpress (MCE) Product Catalog:
Products (202)
202 Results for "binding properties" in MCE Product Catalog:
Cat. No.: HY-G0002S
CAS No.: 2070009-33-3
Cat. No.: HY-N12124
CAS No.: 1011244-19-1
Synonyms: Monascinol
Cat. No.: HY-P5471
CAS No.: 204060-45-7
Synonyms: [Leu27]-Melan-A, MART-1 (26-35)
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Cat. No.: HY-W020012
CAS No.: 78949-95-8
Synonyms: 22-NBD Cholesterol
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Fluoresterol (22-NBD Cholesterol) is a cholesterol-specific fluorescent probe with cholesterol-mimicking binding properties. Fluoresterol is ineffective orally and does not cross the blood-brain barrier. Fluoresterol specifically binds to cholesterol transport-related proteins (such as ABCA1 and ABCG1) and is primarily used in cholesterol metabolism research, particularly for the visualization and quantitative analysis of cholesterol absorption, efflux, intracellular transport efficiency, and reverse cholesterol transport (RCT) processes. The commonly used concentration of Fluoresterol in in vitro experiments is 0.1-10 μM, and the commonly used dose in in vivo experiments is 5-20 mg/kg (gavage or intraperitoneal injection), with excitation/emission wavelengths of 472/540 nm. Fluoresterol can be applied to the study of cholesterol metabolism mechanisms related to hyperlipidemia, atherosclerosis, and non-alcoholic fatty liver disease (NAFLD) .
Cat. No.: HY-L924
1,488 compounds
Boronic acid and boronic ester represent a relatively novel and promising chemical structure in drug design. Boronic acid exists in an sp²-hybridized state, possessing an empty p-orbital that can act as a Lewis acid to accept lone pairs from heteroatoms (O, N, or S). This Lewis acidity enables it to form reversible covalent bonds with amino acid residues such as lysine, serine, threonine, and histidine. Currently, five FDA-approved drugs containing boronic acid or boronic ester predominantly involve such covalent binding mechanisms in their interactions with target proteins. Furthermore, boronic acid can serve as a bioisostere for carboxylic acids, phosphates, and phenolic groups, utilized to improve pharmacokinetic properties and enhance drug efficacy.
To date, five boron-containing drugs have been approved by the FDA. The unique properties of boronic acids and boronic esters confer significant potential in drug design, with applications spanning cancer therapy (e.g., multiple myeloma), anti-infectives (e.g., fungal infections, tuberculosis), anti-inflammatory treatments (e.g., atopic dermatitis), antibacterial agents (e.g., carbapenem-resistant bacterial infections), and Reactive Oxygen Species (ROS)-responsive prodrugs, among others. The MCE Boronic Acid/Boronic Ester Fragment Library, which contains 1,488 compounds, serves as a valuable tool for the development of boron-containing drugs.
Cat. No.: HY-159922
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AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
Cat. No.: HY-19261
CAS No.: 169042-78-8
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T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
Cat. No.: HY-P10427
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Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
Cat. No.: HY-P10427A
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Cat. No.: HY-P1636
CAS No.: 113274-56-9
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Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
Cat. No.: HY-183921
CAS No.: 135100-65-1
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SQ 32547 is a dihydropyridine calcium channel inhibitor with antihypertensive and anti-ischemic activities. SQ 32547 modulates sarcolemmal voltage-dependent calcium channels to inhibit calcium influx, and exerts direct anti-ischemic activity by suppressing myocardial contracture formation and reducing lactate dehydrogenase (LDH) release. SQ 32547 can be used in research related to hypertension, angina pectoris and neurogenic inflammation .
Cat. No.: HY-164429
CAS No.: 2418533-90-9
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
Cat. No.: HY-169798
CAS No.: 23481-50-7
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1,9-Dimethylmethylene blue is a photosensitizer, virus inactivator and hemoglobin oxidant derived from methylene blue. When activated, 1,9-Dimethylmethylene blue generates reactive oxygen species including singlet oxygen, and acts as a metachromatic dye. When activated in monomeric or dimeric form, 1,9-Dimethylmethylene blue induces photoinactivation of R17 phage and vesicular stomatitis virus and oxidizes hemoglobin via non-singlet oxygen reactive oxygen species or singlet oxygen-mediated pathways, respectively. The monomeric form, with higher nucleic acid affinity, achieves virus inactivation under specific conditions without forming methemoglobin. 1,9-Dimethylmethylene blue binds to substances such as glycosaminoglycans to produce color changes. Although it is susceptible to interference from non-glycosaminoglycan components in urine, it is still applicable to spectrophotometric analysis for glycosaminoglycan quantification. With these unique photochemical and binding properties, 1,9-Dimethylmethylene blue is widely used in studies of viral infections and related biochemical analyses .
Cat. No.: HY-W013724
CAS No.: 54735-61-4
Synonyms: IDP disodium; Inosine-5'-diphosphoric acid disodium
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Inosine-5'-diphosphate disodium (IDP disodium) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate disodium has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate disodium abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate disodium has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate disodium can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
Cat. No.: HY-137055
CAS No.: 1171824-96-6
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
Cat. No.: HY-N1970R
CAS No.: 31721-94-5
Category:
other families Flavonoids Phenols Polyphenols Plants Isoflavones
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Cat. No.: HY-W013724S
Synonyms: IDP-15N4 dilithium; Inosine-5'-diphosphoric acid-15N4 disodium
Cat. No.: HY-W020780
CAS No.: 724722-89-8
Synonyms: mPEG5000-Maleimide
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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
