270 Results for "

tolerance

" in MedChemExpress (MCE) Product Catalog:
Products (270)

270 Results for "tolerance" in MCE Product Catalog:

32
32 Cited Publications
Cat. No.: HY-101966
CAS No.: 1916571-90-8
Purity:  99.69%
NCT-503 is a blood-brain barrier-permeable, non-competitive PHGDH inhibitor with an IC50 of 2.5 μM against human PHGDH. NCT-503 reduces glucose-derived serine production and the incorporation of one-carbon units into nucleotides without decreasing PHGDH protein expression. NCT-503 prevents high selenium-induced insulin resistance in mice by regulating blood glucose and insulin levels and improving glucose tolerance, and also inhibits the growth of tumors overexpressing PHGDH. NCT-503 can be used in research related to insulin resistance and breast cancer .
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15
15 Cited Publications
Cat. No.: HY-13991
CAS No.: 285986-88-1
Purity:  99.88%
Target:  

Ras Apoptosis

Research Areas:  

Cancer

CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
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14
14 Cited Publications
Cat. No.: HY-12688A
CAS No.: 864167-45-3
Purity:  ≥98.0%
Succinyl phosphonate trisodium salt is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate trisodium salt protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate trisodium salt corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate trisodium salt reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate trisodium salt improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate trisodium salt can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .
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8
8 Cited Publications
Cat. No.: HY-19870C
CAS No.: 2759937-80-7
Synonyms: RM-493 monoacetate; BIM-22493 monoacetate; IRC-022493 monoacetate
Setmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide monoacetate activates the CaMKK2/AMPK signaling pathway. Setmelanotide monoacetate mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide monoacetate is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression .
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7
7 Cited Publications
Cat. No.: HY-110082
CAS No.: 130-89-2
Quinine hydrochloride is an alkaloid extracted from cinchona bark and exhibits oral activity, acting as a potassium channel inhibitor. Quinine hydrochloride modulates the tolerance of red blood cells and presents dose-dependent toxicity and embryonic effects. Quinine hydrochloride is a typical hemolysin that directly lyses red blood cells, with cellular components of red blood cell membranes as its action targets. Quinine hydrochloride disrupts red blood cell membranes and induces hemolysis at high concentrations, while merely weakening the anti-hemolytic capacity of red blood cells at low concentrations. Quinine hydrochloride continuously reduces red blood cell tolerance after in vivo administration, and high doses can also alter blood cell counts. Quinine hydrochloride can be applied to researches related to red blood cell hemolysis, cancer and malaria .
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6
6 Cited Publications
Cat. No.: HY-121744
CAS No.: 1564265-82-2
Purity:  98.51%
Target:  

PDHK

Research Areas:  

Inflammation/Immunology

PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
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6
6 Cited Publications
Cat. No.: HY-126675A
CAS No.: 2241300-51-4
Purity:  99.94%
Research Areas:  

Inflammation/Immunology

AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4 + T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects .
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6
6 Cited Publications
Cat. No.: HY-126675
CAS No.: 2241300-50-3
Purity:  99.68%
Research Areas:  

Inflammation/Immunology

AS2863619 free base is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 free base targets Stat5a-CDK8/19 to promote the differentiation of CD4 + T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 free base also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 free base exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 free base can be applied to research in related fields such as periodontitis-induced bone defects .
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5
5 Cited Publications
Cat. No.: HY-P1290
CAS No.: 121932-06-7
Synonyms: PKI-(6-22)-amide
Target:  

PKA

Research Areas:  

Neurological Disease

PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing .
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5
5 Cited Publications
Cat. No.: HY-P1290A
Synonyms: PKI-(6-22)-amide TFA
Target:  

PKA

Research Areas:  

Neurological Disease

PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .
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5
5 Cited Publications
Cat. No.: HY-B1329
CAS No.: 65710-07-8
Synonyms: Nebramycin II sulfate
Apramycin (EBL 1003) sulfate is an orally active, acidic pH tolerant and aminoglycoside-modifying-enzymes-tolerant aminoglycoside antibiotic which inhibits protein biosynthesis by targeting the bacterial ribosome. Apramycin sulfate is a potential anti-drug-resistance antibiotic .
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4
4 Cited Publications
Cat. No.: HY-150012
CAS No.: 183241-73-8
Purity:  99.94%
Synonyms: Lac-Phe
N-Lactoyl-phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-phenylalanine can reduce obesity and improve glucose tolerance .
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4
4 Cited Publications
Cat. No.: HY-P99667
CAS No.: 1391727-24-4
Synonyms: OMP-54F28; FZD8-Fc

Target:  

Wnt

Research Areas:  

Cancer

Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
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4
4 Cited Publications
Cat. No.: HY-N2593
CAS No.: 32507-66-7
Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes .
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3
3 Cited Publications
Cat. No.: HY-P0046
CAS No.: 49557-75-7
Synonyms: GHK; Tripeptide-1
Target:  

Peptides

Glycyl-L-histidyl-L-lysine is a tripeptide consisting of glycine, L-histidine and L-lysine residues joined in sequence. Glycyl-L-histidyl-L-lysine is a hepatotropic immunosuppressor and shows anxiolytic effect. Glycyl-L-histidyl-L-lysine and its copper complexes show good skin tolerance .
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3
3 Cited Publications
Cat. No.: HY-P1291
CAS No.: 201422-03-9
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
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3
3 Cited Publications
Cat. No.: HY-P1291A
PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
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3
3 Cited Publications
Cat. No.: HY-N8518
CAS No.: 63335-25-1
Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC50 values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells .
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2
2 Cited Publications
Cat. No.: HY-B0853
CAS No.: 76738-62-0
Research Areas:  

Infection

Paclobutrazol is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins. Paclobutrazol also has antifungal activities. Paclobutrazol, transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants. Paclobutrazol is typically used to support research on the role of gibberellins in plant biology .
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2
2 Cited Publications
Cat. No.: HY-110197
CAS No.: 1774353-12-6
Purity:  99.35%
Target:  

IDE

Research Areas:  

Metabolic Disease

6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes .
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