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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
158 Results for "
elevation
" in MedChemExpress (MCE) Product Catalog:
Products (158)
158 Results for "elevation" in MCE Product Catalog:
Cat. No.: HY-109566R
CAS No.: 2089288-03-7
Synonyms: AZD1390 (Standard)
Research Areas:
Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
Research Areas:
NPS 2390 is an allosteric antagonist of calcium-sensing receptor (CaSR) and mGluR1/5. NPS 2390 inhibits the PI3K/Akt/mTOR signaling pathway, reduces hypoxia-induced intracellular calcium elevation, decreases the expression of autophagy (autophagy) proteins, regulates the expression of phenotypic marker proteins, and inhibits the proliferation of pulmonary artery smooth muscle cells. NPS 2390 attenuates the endogenous apoptosis (apoptosis) pathway, increases the expression level of Bcl-2, downregulates the expression levels of Bax, cytochrome c and caspase-3, alleviates cerebral edema and improves neurological function in rat models. NPS 2390 can be used in studies related to hypoxic pulmonary hypertension, traumatic brain injury, stroke and pain .
Research Areas:
12(R)-HETE is a CYP-dependent arachidonic acid metabolite that acts as a proinflammatory lipid mediator. 12 (R)-HETE widely exists in various tissues including the eye, skin and liver. In the cornea, 12(R)-HETE is metabolized via pathways such as β-oxidation into the precursor of 12(R)-HETrE. Without direct receptor binding, 12(R)-HETE indirectly activates AHR-mediated target gene transcription, while inhibiting the enzymatic activity of Na+,K+-ATPase and the intracellular calcium elevation induced by TP agonists. 12(R)-HETE also possesses multiple physiological effects such as chemotaxis, proangiogenesis, vasodilation, natriuresis, diuresis and intraocular pressure reduction, and can be widely used in studies related to psoriasis, inflammatory skin diseases and ocular inflammation .
Cat. No.: HY-182046
CAS No.: 2930131-74-9
Research Areas:
HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease .
Cat. No.: HY-182677
CAS No.: 221452-76-2
Target:
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EF-7412 is a dual antagonist of the 5-HT1A receptor and dopamine D2 receptor, with Ki values of 27 nM and 22 nM, respectively. EF-7412 acts as an antagonist at both pre- and postsynaptic 5-HT1A receptor sites, blocking 8-OH-DPAT (HY-112061)-induced hypothermia, behavioral syndrome, and corticosterone elevation in vivo. EF-7412 increases hypothalamic 5-HIAA/5-HT and DOPAC/DA ratios, alters 5-HT and DA neuronal activity, and slightly decreases spontaneous motor activity. EF-7412 can be used for research on 5-HT1A/D2 receptor regulation and related neural pathways .
Cat. No.: HY-34464
CAS No.: 136630-39-2
Synonyms: 2,7-DBCZ
Research Areas:
2,7-Dibromocarbazole (2,7-DBCZ) is an orally active AhR agonist and MAOB inhibitor that can cross the blood-brain barrier. 2,7-Dibromocarbazole induces CYP1A/CYP1B1, developmental toxicity and oxidative toxicity, Akt phosphorylation, apoptosis, mitochondrial depolarization, and calcium elevation. 2,7-Dibromocarbazole disrupts dopamine homeostasis, promotes α-synuclein aggregation and transcriptomic dysregulation, leading to hepatic lipid accumulation, liver lesions, brain injury, and angiogenesis/energy metabolism disorders, while activating ERα and inhibiting GRα. 2,7-Dibromocarbazole can be used in research on cardiotoxicity and Parkinson's disease .
Cat. No.: HY-B1035A
CAS No.: 47141-42-4
Synonyms: l-Bunolol
Research Areas:
Levobunolol (l-Bunolol) is a non-selective β-adrenergic antagonist and vasodilator. By blocking calcium ion influx and reducing the sensitivity of vascular smooth muscle to calcium, Levobunolol effectively dilates the ciliary arteries and increases ocular blood flow, so it is widely used in research on glaucoma and ocular hypertension. Levobunolol inhibits the β-receptor signaling pathway and the expression of related proliferation markers (such as CK3, CK14, CK19, Ki67) in corneal cells. In rabbit models, Levobunolol not only does not inhibit corneal epithelial regeneration, but also accelerates the healing of mechanical injury without adverse effects. Levobunolol also inhibits histamine-induced vasoconstriction and intracellular calcium elevation, exhibiting unique vascular regulatory activity. Levobunolol protects ocular blood flow and promotes corneal repair .
Cat. No.: HY-101810R
CAS No.: 82989-25-1
Synonyms: TO 188 (Standard); Tazalest (Standard); Tazanol (Standard)
Target:
Research Areas:
Tazanolast (Standard) (TO 188 (Standard)) is the analytical standard of Tazanolast (HY-101810). This product is intended for research and analytical applications. Tazanolast (TO 188) is an orally active selective mast cell stabilizer. Tazanolast prevents the elevation of intracellular calcium concentration, inhibits calcium uptake and Protein kinase C translocation, without directly inhibiting phospholipase C. Tazanolast inhibits ozone-induced airway hyperresponsiveness to Methacholine in guinea pigs, as well as passive cutaneous anaphylaxis, Schultz-Dale reaction, experimental asthma, passive cutaneous anaphylaxis in rats, and increased cutaneous vascular permeability in rats. Tazanolast does not alter airway responsiveness in sham-exposed guinea pigs, cell distribution in bronchoalveolar lavage fluid after ozone exposure, type II-IV allergic reactions, or histamine release from atopic leukocytes. Tazanolast can be used in research related to allergic diseases .
Cat. No.: HY-N12717
CAS No.: 79786-01-9
Cat. No.: HY-P5142
CAS No.: 193981-10-1
Synonyms: ω-ACTX-Hv1; ω-Atracotoxin-HV1
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Cat. No.: HY-P5142A
Synonyms: ω-ACTX-Hv1 TFA; ω-Atracotoxin-HV1 TFA
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Cat. No.: HY-P992072
Research Areas:
Cat. No.: HY-10952
CAS No.: 357605-73-3
Research Areas:
ONO-AE2-227 is an orally active EP4 receptor antagonist. ONO-AE2-227 blocks PGE2-mediated EP4 signaling by competitively antagonizing PGE2-induced cAMP elevation, and binds to EP4/EP3 with mouse Ki values of 2.7/21 nM. ONO-AE2-227 reduces aberrant crypt foci and intestinal polyp development, and inhibits intestinal polyp formation. ONO-AE2-227 enhances LPS-induced TNF-alpha release from human alveolar macrophages by blocking endogenous PGE2, blocks PGE2-induced ICAM-1 expression and leukocyte-endothelial adhesion, and attenuates PGE2-induced monocyte adhesion to brain endothelial cells. ONO-AE2-227 can be used for research on colon cancer .
Cat. No.: HY-177797
CAS No.: 30439-19-1
Target:
Research Areas:
5-Methoxytryptoline acts as a modulator of the Serotonin transporter complex, as well as a ligand for the 5-HT2A and 5-HT2C receptors, with Ki values of 130 nM and 140 nM for the 5-HT2A and 5-HT2C receptors, respectively. 5-Methoxytryptoline inhibits the active uptake of Serotonin (HY-B1473A) and Tryptamine (HY-B2132) in platelets. 5-Methoxytryptoline induces behavioral excitation, cortical electroencephalographic desynchronization, and dose-dependent elevation of plasma prolactin, followed by behavioral sedation and partial recovery of cortical electroencephalographic voltage. 5-Methoxytryptoline antagonizes Reserpine (HY-N0480)-induced sedation, reduced locomotor activity, and hypothermia. 5-Methoxytryptoline exerts dose-dependent effects on behavior and cortical electroencephalographic activity in freely moving rats. 5-Methoxytryptoline can be used in depression-related research .
Cat. No.: HY-150270
CAS No.: 1239578-79-0
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NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis) .
Research Areas:
NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis) .
Cat. No.: HY-108659
CAS No.: 202982-98-7
Research Areas:
NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal nerve injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation, and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular Ca 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 can be used in the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma .
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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
