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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
956 Results for "
penetrant
" in MedChemExpress (MCE) Product Catalog:
Products (956)
956 Results for "penetrant" in MCE Product Catalog:
Cat. No.: HY-W017540S
Cat. No.: HY-W778990
CAS No.: 478510-94-0
Cat. No.: HY-101349
CAS No.: 156337-32-5
Research Areas:
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
Cat. No.: HY-101349A
CAS No.: 874882-93-6
Research Areas:
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
Cat. No.: HY-104042R
CAS No.: 1644545-52-7
Synonyms: AG-881 (Standard)
Research Areas:
Vorasidenib (Standard) is the analytical standard of Vorasidenib (HY-104042). This product is intended for research and analytical applications. Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
Cat. No.: HY-13324R
CAS No.: 218600-53-4
Synonyms: RTA 402 (Standard); NSC 713200 (Standard); CDDO Methyl ester (Standard)
Research Areas:
Bardoxolone methyl (Standard) is the analytical standard of Bardoxolone methyl (HY-13324). This product is intended for research and analytical applications. Bardoxolone methyl (RTA 402) is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic Kidney disease (CKd) .
Cat. No.: HY-13324S
Synonyms: RTA 402-d3; NSC 713200-d3; CDDO Methyl ester-d3
Research Areas:
Bardoxolone methyl-d3 (RTA 402-d3) is the deuterated-labeled Bardoxolone methyl (HY-13324). Bardoxolone methyl (RTA 402) is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) .
Synonyms: ACT-539313
Research Areas:
Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
Cat. No.: HY-178356
Research Areas:
BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD) .
Cat. No.: HY-189470
Research Areas:
Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy .
Target:
Potassium Channel Cholinesterase (ChE) TRP Channel NOD-like Receptor (NLR) Amyloid-β Tau Protein JNK NF-κB IKK
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
Cat. No.: HY-W027553R
CAS No.: 62732-44-9
Synonyms: NIK-247 free base (Standard); Amiridine free base (Standard)
Research Areas:
Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
Cat. No.: HY-111573R
CAS No.: 1952276-71-9
Synonyms: C286 (Standard)
Target:
Research Areas:
KCL-286 (Standard) is the analytical standard of KCL-286 (HY-111573). This product is intended for research and analytical applications. KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC50 = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC50 = 26 nM) and RAR γ (EC50 = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury .
Cat. No.: HY-175001
Target:
Research Areas:
D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease .
Cat. No.: HY-175532
CAS No.: 3062458-27-6
Target:
Research Areas:
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
Cat. No.: HY-181160
Research Areas:
JNK3/Wnt/β-catenin modulator-1 is a brain-penetrant JNK3 inhibitor and Wnt/β-catenin activator. JNK3/Wnt/β-catenin modulator-1 decreases Aβ1-42 production and reduced ROS generation. JNK3/Wnt/β-catenin modulator-1 inhibits the activation of JNK and Puma, promotes Beclin-1 expression, reduces GSK-3β and BACE1 expression and activates Wnt/β-catenin signaling. JNK3/Wnt/β-catenin modulator-1 improves cognitive and memory performance, attenuates histopathological brain damage, preserves structure of hippocampal pyramidal cells and cerebral cortical neurons. JNK3/Wnt/β-catenin modulator-1 can be used for the research of Alzheimer's disease .
Cat. No.: HY-181613
CAS No.: 3082429-35-1
Target:
Research Areas:
5-HT2A&5-HT2C agonist-3 is an orally active and blood-brain barrier penetrant 5-HT2A and 5-HT2C agonist, with pEC50 values of 7.79 and 7.10, respectively. 5-HT2A&5-HT2C agonist-3 elevates intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used in the research of neuropsychiatric disorders .
Cat. No.: HY-189235
CAS No.: 3078735-55-1
Target:
Research Areas:
IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT2AR and 5-HT2CR agonist (Ki=47.86 nM) that antagonizes 5-HT2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT2AR on enteric glial cells, thereby promoting CD8 + T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT2BR activation. IHCH-8110 exhibits a low risk of hERG channel inhibition (IC50=5.96 μM) and is well tolerated, sensitizing immunologically cold colorectal cancer to PD-1 blockade therapy, making it suitable for research related to colorectal cancer .
Cat. No.: HY-189262
Research Areas:
Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease .
Cat. No.: HY-N1983R
CAS No.: 38395-02-7
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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
