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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
194 Results for "
CSFs
" in MedChemExpress (MCE) Product Catalog:
Products (194)
194 Results for "CSFs" in MCE Product Catalog:
Art. -Nr.: HY-16632
CAS. Nr.: 1333990-84-3
Target:
Forschungsgebiete:
ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease .
Art. -Nr.: HY-114153R
CAS. Nr.: 1303420-67-8
Target:
Forschungsgebiete:
PLX5622 (Standard) is the analytical standard of PLX5622 (HY-114153). This product is intended for research and analytical applications. PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 is an ideal choose for microglia function research in healthy or diseased states. PLX5622 has been verified by MedChemExpress, which demonstrates desirable microglia depletion efficiency in mice. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm .
Art. -Nr.: HY-117854
CAS. Nr.: 141311-11-7
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Forschungsgebiete:
SB 201146 is an LTB4 receptor antagonist with a potency range of 10 pM to 1 μM that plays a critical role in asthma-associated airway inflammation. Studies have focused on its effects on eosinophil survival, a hallmark of asthma pathology. Studies have shown that eosinophil-derived cysteinyl leukotrienes, including LTC4 and LTD4, as well as factors such as GM-CSF and fibronectin promote eosinophil survival. SB 201146 effectively reversed mast cell- and lymphocyte-induced eosinophil survival, highlighting its potential therapeutic role in disrupting the autocrine cysteinyl leukotriene pathway that maintains eosinophil viability. This antagonist also highlights the importance of LTB4 as a paracrine mediator that influences eosinophil survival in inflammatory settings such as asthma .
Art. -Nr.: HY-148527
CAS. Nr.: 1347232-69-2
Synonyms: AZD8999
Forschungsgebiete:
LAS190792 is a bifunctional muscarinic acetylcholine receptor (mAChR) antagonist and β2-adrenergic receptor agonist. LAS190792 has a pIC50 of 8.8 against human M3 muscarinic receptor and a pIC50 of 9.1 against human β2-adrenergic receptor. LAS190792 exhibits vasodilatory and anti-inflammatory activities, and induces sustained bronchodilation in dogs. LAS190792 inhibits the release of IL-8, MMP9, IL-1β and GM-CSF from lipopolysaccharide-stimulated neutrophils. LAS190792 can be used in research related to respiratory system diseases .
Art. -Nr.: HY-152830A
Reinheit: 99.82%
Synonyms: Q702 TFA
Target:
Forschungsgebiete:
Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
Art. -Nr.: HY-159838
CAS. Nr.: 2222689-47-4
Synonyms: EI‐1071
Forschungsgebiete:
Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer .
Art. -Nr.: HY-16633
CAS. Nr.: 1444006-79-4
Target:
Forschungsgebiete:
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .
Art. -Nr.: HY-183931
CAS. Nr.: 1839155-15-5
Target:
Forschungsgebiete:
NPA101.3 is an orally active RET receptor tyrosine kinase and VEGFR2 inhibitor (RET IC50 = 0.001 μM, RET V804M IC50 = 0.008 μM, VEGFR2 IC50 = 0.003 μM). NPA101.3 inhibits purified TRKA (IC50 = 32 nM) and CSF1R (IC50 = 46 nM). NPA101.3 completely suppresses tumor formation in RET /C634Y-transformed cells and also attenuates tumor formation in HRAS /G12V-transformed cells. NPA101.3 can be used in the research of RET-driven cancers .
Art. -Nr.: HY-101034
CAS. Nr.: 2081093-21-0
Synonyms: CHMFL-ABL-KIT-155
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
Art. -Nr.: HY-149465
CAS. Nr.: 2298391-60-1
Target:
Forschungsgebiete:
STF-1623 is a highly potent, selective, cell-impermeable non-covalent ENPP1 inhibitor, with IC50 values of 0.6 nM and 800 nM against human ENPP1 and ENPP3, respectively. STF-1623 inhibits the hydrolysis of extracellular cGAMP by ENPP1, elevates intratumoral cGAMP levels, and indirectly enhances local cGAS-STING signaling and anti-tumor immunity in tumors. STF-1623 exhibits target-dependent retention in ENPP1-highly expressing tumors, while it undergoes rapid clearance in systemic circulation, and can penetrate into the CSF and brain parenchyma. STF-1623 can be used in studies related to breast cancer, pancreatic cancer, colorectal cancer, glioblastoma, and tumor immunology .
Art. -Nr.: HY-164529
CAS. Nr.: 2121503-76-0
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
Art. -Nr.: HY-W583212
CAS. Nr.: 14354-67-7
Synonyms: ZnMP
Synonyms: TT 00420
Target:
Forschungsgebiete:
Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment .
Art. -Nr.: HY-186072
CAS. Nr.: 2771019-10-2
Forschungsgebiete:
Neurological Disease Metabolic Disease Inflammation/Immunology
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
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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
