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KARI 201

  Cat. No.:  DC70536   Featured
Chemical Structure
2376132-22-6
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More than 5000 active chemicals with high quality for research!
Field of application
KARI-201 is a multifunctional small molecule that demonstrates dual activity as a highly selective inhibitor of acid sphingomyelinase (ASM) and an agonist of the ghrelin receptor. It operates as a competitive inhibitor by binding directly to the active site of ASM. Studies reveal that the incorporation of KARI-201 into ASM decreases in a concentration-dependent manner with sphingomyelin, resulting in KM values of 332.5, 433.9, and 572.6 μM at KARI-201 concentrations of 1, 10, and 100 μM, respectively. In preclinical models, KARI-201 has shown efficacy in reducing amyloid pathology and reversing cognitive deficits in APP/PS1 mice. Additionally, it enhances autophagy degradation by promoting lysosomal biogenesis in neuronal cells. As a ghrelin receptor agonist, KARI-201 also supports hippocampal neurogenesis and improves synaptic plasticity, making it a promising therapeutic candidate for neurodegenerative conditions.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2376132-22-6
Chemical Name: KARI 201
Synonyms: KARI-201
Formula: C14H28N4O2
M.Wt: 284.404
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC70634 N8279 N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible allosteric activity, which could be competitively inhibited by GHSR1a antagonists YIL781 and JMV2959.N8279 is a weak activator of GHSR1a-mediated, βarr2-dependent cellular responses relative to ghrelin.N8279 requires receptor sites and/or conformational states driven by the GHSR1a ECD that are distinct from ghrelin.N8279 is brain-penetrant and attenuates aberrant DAergic behavior in mice.
DC70536 KARI 201 KARI-201 is a multifunctional small molecule that demonstrates dual activity as a highly selective inhibitor of acid sphingomyelinase (ASM) and an agonist of the ghrelin receptor. It operates as a competitive inhibitor by binding directly to the active site of ASM. Studies reveal that the incorporation of KARI-201 into ASM decreases in a concentration-dependent manner with sphingomyelin, resulting in KM values of 332.5, 433.9, and 572.6 μM at KARI-201 concentrations of 1, 10, and 100 μM, respectively. In preclinical models, KARI-201 has shown efficacy in reducing amyloid pathology and reversing cognitive deficits in APP/PS1 mice. Additionally, it enhances autophagy degradation by promoting lysosomal biogenesis in neuronal cells. As a ghrelin receptor agonist, KARI-201 also supports hippocampal neurogenesis and improves synaptic plasticity, making it a promising therapeutic candidate for neurodegenerative conditions.
DC44099 Capromorelin tartrate Capromorelin Tartrate (CP 424391-18), a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki of 7 nM for hGHS-R1a and EC50 of 3 nM for rat pituicyte.
DC11246 Ghrelin agonist HM01 Ghrelin agonist HM01 is a novel potent, orally available ghrelin (GHS-R) agonist with Ki of 1.42 nM (human GHS-R1a), induces potent activation of intracellular calcium signaling with EC50 of 1.25 nM.
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