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4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mousebrain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
4-tert-Octylphenol (Standard) is the analytical standard of 4-tert-Octylphenol. This product is intended for research and analytical applications. 4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mousebrain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mousebrain. MCOPPB is used in anxiety disorders research .
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mousebrain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mousebrain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mousebrain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mousebrain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent .
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases .
Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .
GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mousebrain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant .
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .
Firazorexton hydrate (TAK-994) is a potent, brain-penetrant, and orally active orexin type 2 receptor (OX2R) agonist (EC50: 19 nM). Firazorexton hydrate inhibits fragmentation of wakefulness and cataplexy-like episodes in mouse models of narcolepsy .
Halocyamine B exhibits antimicrobial activity against a variety of bacteria and yeasts. Halocyamine B exhibits cytotoxicity to cultured neural cells of rat fetal brain, mouse neuroblastoma N18 cells, and human hepatoma HepG2 cells .
MS152 is an oral bioactive inhibitor of EHMT2/G9a. MS152 reactivats maternally silenced Prader-Willi syndrome (PWS) genes in brain and liver tissues of PWS mouse models .
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
LP-403812 is a high affinity proline transporter (PROT) inhibitor that produces dose-dependent inhibition of hPROT (IC50=0.11 μM; Ki=0.12 μM) and also inhibits the activity of mousebrain synaptosomal mPROT with the same potency (IC50=0.23 μM). LP-403812 can be used to study the function of PROT in the brain .
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mousebrain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mousebrain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mousebrain .
FFN246 is a fluorescent, dual substrate of serotonin transporter (SERT) probe and vesicular monoamine transporter 2 (VMAT2) with excitation and emission spectra 392/427 nm. FFN246 can be used for labeling serotonergic neurons in mousebrain tissue through SERT-dependent accumulation .
Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mousebrain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
Racecadotril (Standard) is the analytical standard of Racecadotril. This product is intended for research and analytical applications. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mousebrain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent .
Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research .
S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [ 3H]CP-55940 to the CB1 receptor (IC50: 19.31 μM) .
Docosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system .
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R . TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively .
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50=34.1 nM). It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg/kg) increases levels of 2-arachidonoyl glycerol in mousebrain.
C2 3'-Sulfo galactosylceramide (d18:1/2:0) (C2 Sulfatide) is one of the sulfatide class of glycolipids. C2 3'-Sulfo galactosylceramide (d18:1/2:0) can be used in the quantification of lysosulfatides in mousebrain tissue and plasma .
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
KP-302 (compound 23) is a selective inhibitor of protein arginine deaminase PAD2 with a Ki of 60 μM. KP-302 also reversed physical disability in the EAE mouse model of multiple sclerosis (MS) and eliminated T cell infiltration in the brain. KP-302 has the potential to be a disease-modifying agent for MS .
Ethiprole (Standard) is the analytical standard of Ethiprole. This product is intended for research and analytical applications. Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mousebrain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
FTY720-C2 is a derivative of FTY72 (HY-12005). FTY720-C2 promotes the expression of brain-derived neurotrophic factor (BDNF) and glial cell-derived neurotrophic factor (GDNF) in multiple system atrophy (MSA) models, without causing immunosuppression. FTY720-C2 improves motor dysfunction and reduces the levels of insoluble alpha-synuclein (αSyn) in MSA mouse models. FTY720-C2 is blood-brain barrier penetrate .
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mousebrain .
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
Hydroxy Dynasore (Dyngo-4a), a structural mimetic analog of Dynasore (HY-15304), is an improved, less cytotoxic and versatile dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain recombinant dynamin I and recombinant mouse dynamin II, respectively. Hydroxy Dynasore inhibits dynamin-dependent transferrin endocytosis with an IC50 of 5.7 μM.
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
LK-2 is an antagonist for ASIC1a with a Kd of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC50 of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable .
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mousebrain membranes .
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable .
JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research .
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouseconstitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouseconstitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouseconstitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
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 .
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mousebrain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mousebrain .
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD .
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice .
RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mousebrain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC50 values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease .
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable .
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research .
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
Brain Natriuretic Peptide-45, mouse (BNP-45, mouse) is a circulating form of mousebrain natriuretic peptide isolated from mouse heart with potent hypotensive and natriuretic potency .
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mousebrain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mousebrain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
[D-Arg2]Dermorphin-(1-4) amide is a N-terminal shorter peptide amide of [D-Arg2]dermorphin with the hypothermic effect. [D-Arg2]Dermorphin-(1-4) amide shows analgesic activity and degradation in soluble mouse liver and brain extracts .
CAQK peptide selectively binds to injured mousebrain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mousebrain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mousebrain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mousebrain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
4-tert-Octylphenol (Standard) is the analytical standard of 4-tert-Octylphenol. This product is intended for research and analytical applications. 4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mousebrain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
Halocyamine B exhibits antimicrobial activity against a variety of bacteria and yeasts. Halocyamine B exhibits cytotoxicity to cultured neural cells of rat fetal brain, mouse neuroblastoma N18 cells, and human hepatoma HepG2 cells .
Docosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system .
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
Brain Derived Neurotrophic Factor (BDNF) is a neurotrophin that belongs to NGF-beta family. BDNF can bind to its high affinity receptor TrkB and activates signal transduction cascades (IRS1/2, PI3K, Akt). BDNF can also bind to the p75NTR, but the affinity for the p75NTR receptor is lower than for TrkB. BDNF is a neurotransmitter modulator, and is vital in maturation, survival and differentiation of neuronal populations during development. BDNF also participates in neuronal plasticity, which is essential for learning and memory. BDNF is widely expressed in the CNS. BDNF Protein, Mouse (R129A, R130A, HEK293, His) is a recombinant mouse BDNF (M1-R249, R129A, R130A) with C-terminal His tag, which is produced in HEK293.
BDNF protein is an important signaling molecule that activates NTRK2 downstream cascades and affects multiple roles in neuronal development and function. It promotes survival and differentiation of the peripheral and central nervous system, affecting axonal and dendritic growth. BDNF Protein, Mouse (R129A, R130A, HEK293, C-His) is the recombinant mouse-derived BDNF protein, expressed by HEK293 , with C-6*His labeled tag and R129A, R130A, , , mutation. The total length of BDNF Protein, Mouse (R129A, R130A, HEK293, C-His) is 231 a.a., with molecular weight of ~35-42 kDa.
Pleiotrophin (PTN) is a secreted growth factor that transduces signals through cell surface proteoglycan and non-proteoglycan receptors.PTN binds to chondroitin sulfate (CS) groups and regulates cell proliferation, survival, and differentiation, particularly inhibiting long-term synaptic potentiation of neurons.Pleiotrophin Protein, Mouse (HEK293, His) is the recombinant mouse-derived Pleiotrophin protein, expressed by HEK293 , with C-6*His labeled tag.
CNTN4/Contactin-4 protein mediates cell surface interactions in nervous system development and promotes neurite outgrowth. Its involvement in synaptogenesis highlights its significance in shaping neural connectivity. CNTN4 also interacts with PTPRG, potentially regulating neuronal functions and synaptic development. CNTN4/Contactin-4 Protein, Mouse (sf9, His) is the recombinant mouse-derived CNTN4/Contactin-4 protein, expressed by Sf9 insect cells , with C-His labeled tag.
Endoglycan/PODXL2 Protein serves as a ligand for vascular selectins, enabling leukocyte rolling on vascular surfaces via high affinity interactions with E-, P-, and L-selectins. It exists as a disulfide-linked homodimer. Furthermore, Endoglycan/PODXL2 Protein interacts with SELL, SELE, and SELP, enhancing its role in leukocyte adhesion and trafficking in the vasculature. Endoglycan/PODXL2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Endoglycan/PODXL2 protein, expressed by HEK293 , with C-His labeled tag.
CES3/CES1D Protein, a major lipase in white adipose tissue, plays a crucial role in xenobiotic and natural substrate metabolism. It hydrolyzes triacylglycerols and monoacylglycerols, showing a preference for the latter, with susceptibility increasing as the acyl chain length decreases. Additionally, CES3/CES1D catalyzes the synthesis of fatty acid ethyl esters and hydrolyzes retinyl esters. CES3/CES1D Protein, Mouse (HEK293, His) is the recombinant mouse-derived CES3/CES1D protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CES3/CES1D Protein, Mouse (HEK293, His) is 543 a.a., with molecular weight of 58-70 kDa.
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mousebrain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
Ulefnersen sodium (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen sodium can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen sodium can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
Ulefnersen (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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