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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
36 Results for "
weak base
" in MedChemExpress (MCE) Product Catalog:
Products (36)
36 Results for "weak base" in MCE Product Catalog:
Cat. No.: HY-111259
CAS No.: 81228-35-5
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Ro 31-1118 Free base is a compound exhibiting weak antihypertensive activity in patients with mild hypertension. Ro 31-1118 Free base demonstrated a reduction in heart rates and blood pressure post-exercise at varying doses. Ro 31-1118 Free base exhibited linear pharmacokinetics within the 10-80 mg dose range. Ro 31-1118 Free base showed no significant impact on diastolic blood pressure or adverse effects during the study.
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Copper(I) oxide is a weak inorganic base, oxidative stress inducer and cytotoxic agent. Copper(I) oxide generates ROS by impairing the activities of Catalase (HY-135849) and glutathione reductase. Copper(I) oxide can be used to activate halides for nucleophilic substitution reactions, and is also suitable for decarboxylation and ring condensation reactions .
Cat. No.: HY-105525
CAS No.: 143257-97-0
Synonyms: NIH 10908 free base
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Sameridine (NIH-10908 free base) is a weak partial agonist of the μ-opioid receptor. Sameridine shows local anesthetic and analgesic properties. Sameridine has minimal respiratory depression at low doses, but can suppress ventilatory response at high doses. Sameridine can be used for the study of analgesic effect .
Cat. No.: HY-N15947
CAS No.: 2089062-80-4
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Trifunctional sphingosine is a clickable sphingoid base derivative. Trifunctional sphingosine can be used to study the biological function of sphingoid bases. Trifunctional lipids may overcome several challenges in interrogating lipid biology: their fast metabolism, their weak and transient (but functionally important) interactions with proteins, and the difficulty in tagging them without disturbing the cellular location .
Cat. No.: HY-W075283
CAS No.: 919789-80-3
Synonyms: 1-(4-Aminophenyl)-1,2,2-triphenylethene
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4-(1,2,2-Triphenylvinyl)aniline (1-(4-Aminophenyl)-1,2,2-triphenylethene) is a tetraphenylethene-based aggregation-induced luminescent molecule. 4-(1,2,2-Triphenylvinyl)aniline exhibits weak or no fluorescence in dilute solution/dispersed state, and strong fluorescence with increased quantum yield when aggregated into nanoparticles .
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Cat. No.: HY-19153A
CAS No.: 157564-11-9
Synonyms: rel-TY-11345
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Nepaprazole sodium (rel-TY-11345) is a proton pump H+/K+-ATPase inhibitor. Nepaprazole sodium inhibits H+/K+-ATPase activity in rabbit gastric mucosal microsomes, with IC50 values of 5.8 μM and 9.9 μM at pH 6.0 and pH 7.4, respectively, and its inhibitory activity is enhanced under weakly acidic conditions. Nepaprazole sodium inhibits basal and Tetragastrin (HY-125556)-stimulated gastric acid secretion. Nepaprazole sodium can be used in studies on gastric proton pump function, gastric acid secretion, and mechanisms related to peptic ulcers .
Cat. No.: HY-29358
CAS No.: 72391-21-0
2-Aminoethanol,4-(2,5,7,7-tetramethyloctan-4-yl)benzenesulfonic acid is a triethanolammonium-based salt with weak antiproliferative, anti-angiogenic, and antibacterial activity. 2-Aminoethanol,4-(2,5,7,7-tetramethyloctan-4-yl)benzenesulfonic acid acts on cancer cells, inhibits endothelial cell migration, and targets Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumoniae. 2-Aminoethanol,4-(2,5,7,7-tetramethyloctan-4-yl)benzenesulfonic acid can be used for the research of breast cancer and bacterial infections .
Cat. No.: HY-185985
CAS No.: 3113145-60-8
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Am-Ka12K4 is a weakly positively charged peptide-based ionizable lipid. Am-Ka12K4 induces membrane disruption under endosomal pH conditions and possesses high lipid fusion capacity. Am-Ka12K4 forms tightly packed, stable lipid nanoparticles. Am-Ka12K4 mediates in vivo mRNA delivery, exhibits inherent liver tropism, and can be modified to adjust organ tropism, enabling selective mRNA delivery to the spleen, lung, or thymus. Am-Ka12K4 is applicable to research related to repetitive mild traumatic brain injury .
Cat. No.: HY-D3117
CAS No.: 2146114-18-1
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MBCB is a two-photon Fluorescent probe for dual-detection of mitochondrial SO₂ derivatives and viscosity. For SO₂ derivatives detection, the probe utilizes a Michael addition mechanism: nucleophilic addition of SO₂ derivatives to the C=C bond between the carbazole skeleton and 3-methylbenzothiazolium moiety destroys the strong intramolecular charge transfer (ICT) system between these groups, while enhancing the weak ICT system between the benzothiazole group and carbazole framework; this causes the red emission at 600 nm to decrease and the blue emission at 434 nm to increase, creating a ratiometric response based on the I₄₃₄ₙₘ/I₆₀₀ₙₘ intensity ratio. For viscosity detection, in low-viscosity environments, steric hindrance creates a twisted ICT (TICT) system with weak fluorescence, while in high-viscosity environments, intramolecular rotation is blocked, the TICT state is disrupted, and the strong ICT system is recovered, leading to a strong red emission at 567 nm with negligible change to the short-wavelength emission at 415 nm, creating a ratiometric response based on the I₅₆₇ₙₘ/I₄₁₅ₙₘ intensity ratio that has a logarithmic linear relationship with viscosity. The probe has excitation/emission wavelengths of Ex/Em = 351/434, 600 nm for SO₂ derivatives detection and Ex/Em = 351/567 nm for viscosity detection, with two-photon excitation at 740 nm for bioimaging; it also exhibits good mitochondrial targeting ability with a Pearson's colocalization coefficient of 0.93 when paired with Mito-Tracker Green. The probe shows high sensitivity and selectivity for SO₂ derivatives, has low cell cytotoxicity, and can be applied to detect exogenous/endogenous HSO₃⁻ in living cells and in vivo, as well as visualize mitochondrial viscosity changes induced by nystatin[1].
Cat. No.: HY-185899
CAS No.: 72052-96-1
Synonyms: 5-Aza-2'-deoxycytidine-5′-triphosphate
5-Aza-dCTP (5-Aza-2'-deoxycytidine-5′-triphosphate) is a nucleotide analog that acts as a substrate for mammalian DNA polymerase α (Km = 3.0 μM) and a weak competitive inhibitor of this enzyme (Ki = 4.3 μM). 5-Aza-dCTP inhibits DNA polymerase α via incorporation into DNA through Watson-Crick base pairing, inhibits DNA methyltransferases via incorporation into hemimethylated DNA, and induces mutations in HIV-1 via incorporation into viral DNA during synthesis. 5-Aza-dCTP reverses the inhibitory effect of dTTP on dCMP deaminase, and allosterically activates dCMP deamination to the same extent as dCTP. 5-Aza-dCTP is applicable to research related to leukemia and type 1 human immunodeficiency virus infection .
Cat. No.: HY-D3086
CAS No.: 1668565-72-7
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Mito-polarity is a mitochondria-targeted polarity probe. Mito-polarity can be used to detect mitochondrial polarity. The detection mechanism of Mito-polarity is based on an intramolecular charge transfer (ICT) system designed with a donor-π-bridge-acceptor (D-π-A) structure. Among them, the 467 nm green emission generated by the Coumarin (HY-N0709) structure is extremely sensitive to polarity changes, while the 642 nm red emission produced by the extended π-conjugation and ICT effect between the Coumarin and benzothiazine structures shows only a weak response, thus forming a ratiometric fluorescence response that is linearly correlated with solvent polarity. When Mito-polarity is excited at 405 nm in methanol, its excitation/emission wavelengths are Ex/Em = 405/467 nm and Ex/Em = 405/642 nm, with maximum absorption wavelengths of 426 nm and 561 nm .
Cat. No.: HY-P11899
Synonyms: Cyclo(VVIaWG)
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Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) (Cyclo(VVIaWG)) is a six-membered cyclic peptide designed based on the C-terminal region of Aβ1-42. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) binds selectively to Aβ15-36 (Kd = 0.6 μM), regulates the aggregation of Aβ1-42 at high concentrations, weakly inhibits fibrillation at a 10-fold excess, and inhibits oligomerization at equimolar concentrations. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) does not interfere with the aggregation of IAPP. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) can serve as a targeting ligand for fluorescent probes of Aβ prefibrillar aggregates, and is applicable to research related to Alzheimer's disease .
Cat. No.: HY-D3119
CAS No.: 2246946-49-4
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MitoAIE1 is a Fluorescent probe for mitochondrial viscosity detection. MitoAIE1 contains a pyridinium structural unit, which endows it with mitochondria-targeting specificity. The detection mechanism of this probe is based on aggregation-induced emission (AIE): in low-viscosity media such as PBS buffer, intramolecular rotation leads to non-radiative energy dissipation, resulting in only weak fluorescence; however, in high-viscosity environments such as the mitochondrial matrix or the vicinity of the inner mitochondrial membrane, such intramolecular motion is restricted, thereby significantly enhancing its fluorescent signal; in addition, this probe is not interfered by changes in microenvironment polarity and pH. Its emission wavelength is 625 nm, with absorption peaks at 325 nm and 450 nm; when transferred from low-viscosity PBS to high-viscosity 99% glycerol, its fluorescence intensity at 625 nm can be increased by 38-fold. It can be used to monitor changes in mitochondrial viscosity during processes such as Stauroporine (HY-15141)-induced apoptosis and starvation-induced mitophagy in live cells, and has good biocompatibility .
Cat. No.: HY-182354
CAS No.: 861877-12-5
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
Cat. No.: HY-L942
1,626 compounds
Unlike highly conserved orthosteric sites, allosteric sites exhibit low conservation, high hydrophobicity, weak polarity, confined geometry, and dynamic cryptic properties. Rather than rigid keyhole-like cavities, they typically appear as flexible grooves, subunit interface clefts, or shallow depressions formed by protein conformational changes.
Based on the dynamic, hydrophobic, and elongated nature of allosteric pockets, MCE has carried out targeted fragment modification and screening under strict physicochemical criteria: MW 120–280 Da, HBD ≤ 2, HBA ≤ 3, PSA 30–80 Ų, rotatable bonds ≤ 2, cLogP 1–3.5. High 3D diversity was further ensured by PMI analysis, yielding fragments with excellent shape complementarity to allosteric pockets.
This library contains 1,800 structurally diverse, drug-like fragments, this library supports allosteric drug development and pocket optimization. It significantly improves screening hit rates and enables efficient, precise early-stage R&D of allosteric drugs.
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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
