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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
2046 Results for "
concentrations
" in MedChemExpress (MCE) Product Catalog:
Products (2046)
2046 Results for "concentrations" in MCE Product Catalog:
Cat. No.: HY-113416AS
Purity: 98.00%
Synonyms: DHEA sulfate-d6 sodium dihydrate; Prasterone sulfate-d6 sodium dihydrate
Cat. No.: HY-117219
CAS No.: 136209-43-3
Research Areas:
SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
Cat. No.: HY-121642
CAS No.: 1169831-01-9
SL-017 is a novel photoacoustic sensitizer and a derivative of photofrin B. It can be taken up by cells to the maximum extent within 30 minutes and is mainly localized in mitochondria. After being activated by visible light or ultrasound, SL-017 can significantly increase the production of reactive oxygen species (ROS). Low concentrations of SL-017 can rapidly cause the loss of mitochondrial membrane potential. SL-017 can also cause mitochondrial fragmentation, a process that occurs after the loss of membrane potential. Epoxyeicosatrienoic acids (EETs) can alleviate the loss of mitochondrial membrane potential caused by SL-017, but the antioxidant ascorbic acid has no such effect. These characteristics indicate that SL-017 mainly targets mitochondria and exerts its cytotoxic effect by triggering the collapse of mitochondrial membrane potential, generating ROS, and causing mitochondrial fragmentation. As a novel photoacoustic sensitizer, SL-017 has potential application value in photodynamic therapy and sonodynamic therapy.
Cat. No.: HY-12688
CAS No.: 26647-82-5
Research Areas:
Chlorpromazine (Standard) is the analytical standard of Chlorpromazine (HY-12708). This product is intended for research and analytical applications. Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
Cat. No.: HY-13527A
CAS No.: 379215-96-0
Target:
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LY310762 free base is a selective 5-HT1D receptor antagonist with a Ki value of 249 nM for the guinea pig receptor. LY310762 free base blocks presynaptic 5-HT1D autoreceptors and enhances potassium-stimulated [ 3H]5-HT outflow from guinea pig cortical slices. LY310762 free base abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT1D receptors. LY310762 free base potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 free base is used in research related to depression and diabetic nephropathy .
Cat. No.: HY-136720
CAS No.: 304913-22-2
ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
Cat. No.: HY-138074
CAS No.: 93074-04-5
Synonyms: 5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
Cat. No.: HY-145425
CAS No.: 2771006-54-1
Research Areas:
PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis .
Cat. No.: HY-14988
CAS No.: 1143579-76-3
I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids (5a–u), exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N-(1-adamantyl)-2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N-(1-adamantan-1-yl)-2-(4-(phenanthren-2-yl)-1H-1,2,3-triazol-1-yl)acetamide (5t) showed the most promise with a minimum inhibitory concentration (MIC) of 3.12 μg/mL against Mycobacterium tuberculosis H37Rv, and a selectivity index greater than 15 .
Cat. No.: HY-152021S
CAS No.: 2692624-25-0
Target:
Research Areas:
C18 Ceramide-1-phosphate (d18:1/18:0)-d3 is the deuterium labeled C18 Ceramide-1-phosphate (d18:1/18:0) (HY-160850). C18 Ceramide-1-phosphate (d18:1/18:0) is a specific type of long-chain molecule found in murine skin. C18 Ceramide-1-phosphate (d18:1/18:0) promotes migration of both mouse bone marrow-derived multipotent stromal cells and human umbilical vein endothelial cells at concentrations between 0.5-5 μM. C18 Ceramide-1-phosphate (d18:1/18:0)’s levels are higher in CFPAC-1 pancreatic ductal adenocarcinoma cells than in pancreatic cancer stem cells .
Cat. No.: HY-156807
CAS No.: 210751-39-6
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LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
Cat. No.: HY-178984
CAS No.: 3095278-75-1
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PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
Cat. No.: HY-181588
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Research Areas:
NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis .
Cat. No.: HY-183403
CAS No.: 457075-21-7
Synonyms: CHF 2819 free base
Target:
Research Areas:
Ganstigmine (CHF 2819 free base) is a potent, orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor, with an IC50 value of 65 nM against human AChE, 310 nM against human butyrylcholinesterase (BChE), and 5.12 μM against Torpedo californica AChE. Ganstigmine increases extracellular acetylcholine levels in the brain of rodents without altering the concentrations of other neurotransmitters, stimulates cholinergic transmission, and induces the release of soluble non-amyloidogenic amyloid precursor protein. Ganstigmine exhibits neuroprotective activity independent of cholinesterase inhibition, prevents neuronal death, alleviates β-amyloid-induced neurodegeneration, rescues cholinergic neuron loss, and reverses Scopolamine (HY-N0296)-induced amnesia and memory deficits. Ganstigmine shows cholinesterase inhibition-independent neuroprotective effects against growth factor deprivation and Aβ25-35 toxicity. Ganstigmine can be used in research on Alzheimer's disease, cholinergic dysfunction, and neuroprotection .
Cat. No.: HY-B0407AR
CAS No.: 69-09-0
Research Areas:
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
Cat. No.: HY-D1056B1
Synonyms: LPS, from bacterial (Proteus vulgaris)
It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
Cat. No.: HY-D3003
CAS No.: 2522921-17-9
Cat. No.: HY-D3074
Target:
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TCM-4COOH is an AIE-active fluorescent probe for calcium ions. TCM-4COOH relies on aggregation-induced emission activity, and its carboxyl chelating group can bind to Ca 2+ and Mg 2+ to form insoluble aggregates, triggering fluorescence enhancement via restricting intramolecular motion (Ex/Em = 477/603 nm). TCM-4COOH shows pH independence in physiological environments (pH 4-9), can be strongly activated at Ca 2+ concentrations ranging from low nM to mM, and has a stronger binding ability to Ca 2+ than to Mg 2+. TCM-4COOH, as its acetoxymethyl ester derivative TCM-AM, can penetrate cell membranes for intracellular detection. TCM-4COOH can be used for imaging of cellular calcium overload, detection of bone microcracks, and studies related to calcium-rich biological environments .
Cat. No.: HY-D3148
CAS No.: 1804107-88-7
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TPE-Ph-In is a mitochondria-targeted voltage-sensitive probe that can be used for mitochondrial membrane potential detection, mitochondrial imaging of animal and plant cells and tissues, mouse sperm activity indication, and detection of mitochondrial membrane potential changes associated with early apoptosis. TPE-Ph-In is non-fluorescent in solution, but emits strong fluorescence when aggregated via restriction of intramolecular rotation/movement, and its fluorescence intensity is directly correlated with local probe concentration or mitochondrial membrane potential level. TPE-Ph-In can penetrate cell membranes, target mitochondria through charge-dependent accumulation, has low cytotoxicity and high photostability, and enables super-resolution imaging of plant mitochondrial fission, fusion and cristae structures. The excitation wavelengths of TPE-Ph-In include 450 nm, 488 nm, and 489 nm, while its emission wavelengths include 551-661 nm, 660 nm, and 694 nm. TPE-Ph-In can be used for studies on mitochondrial dysfunction associated with early apoptosis .
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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
