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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
123 Results for "
penetration inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (123)
123 Results for "penetration inhibitor" in MCE Product Catalog:
77
77 Publications Verification
Synonyms: GS 4071; Ro 64-0802; Oseltamivir carboxylate
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Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
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44 Cited Publications
Synonyms: CH5424802; RO5424802; RG7853
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Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
44
44 Cited Publications
Synonyms: CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
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Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
7
7 Cited Publications
Synonyms: 2-(Phosphonomethyl)pentanedioic acid
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2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases .
7
7 Cited Publications
Cat. No.: HY-17595
CAS No.: 31431-39-7
Target:
Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
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7 Cited Publications
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URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
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7 Cited Publications
Cat. No.: HY-100788C
CAS No.: 373645-42-2
Synonyms: 2-(Phosphonomethyl)pentanedioic acid sodium
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2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases .
3
3 Cited Publications
Cat. No.: HY-B0848
CAS No.: 41814-78-2
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Tricyclazole is a pentaketone melanin biosynthesis inhibitor and a unique fungicide for controlling rice blast. Tricyclazole alters the structure and function of fungal cell walls, reduces fungal pathogenicity and penetration, and causes dose-dependent liver damage in animals .
3
3 Cited Publications
Synonyms: EXP999; RP9965
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Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
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2 Cited Publications
Cat. No.: HY-16712
CAS No.: 1627503-67-6
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LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
1
1 Cited Publications
Cat. No.: HY-N2345
CAS No.: 23567-23-9
1
1 Cited Publications
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BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases .
1
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
1
1 Cited Publications
Cat. No.: HY-W395779
CAS No.: 1335113-30-8
EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM .
1
1 Cited Publications
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(S)-SNAP5114 is a non-covalent murine GABA transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC50=5.71, pKi=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases .
Synonyms: Anle138b
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Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
Cat. No.: HY-148811
CAS No.: 2403703-30-8
Synonyms: ICP-723
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Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
Cat. No.: HY-175715
CAS No.: 3077720-24-9
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NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease .
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MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration .
Cat. No.: HY-164782
CAS No.: 2710273-81-5
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PT3 is a selective inhibitor of HDAC3 with an IC50 value of 0.25 μM. PT3 exhibits good brain penetration ability and bioavailability upon oral administration. PT3 can be used in the research of Alzheimer’s disease .
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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
