Neurotransmission, neural targets and neurological research.
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CAS 130929-57-6
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.IC50 Value: 151 nMTarget: COMTin vitro: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in…
CAS 803735-54-8
AZ-1 is a small molecule inducer of ABCA1 and apoE that act through indirect activation of the LXR pathway, shows purinergic receptor P2X7 antagonist activity; upregulates ABCA1 across multiple CNS cell types, including human astrocytes, pericytes, and…
CAS 934240-30-9
CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus…
CAS 1346133-08-1
LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]Target: κ-opioid Receptorin vitro: LY2795050 displays…
CAS 634908-75-1
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 nM for 5-HT.
CAS 1313498-08-6
LSN2814617 is a neurotoxic positive allosteric modulator. For the detailed information of LSN2814617, the solubility of LSN2814617 in water, the solubility of LSN2814617 in DMSO, the solubility of LSN2814617 in PBS buffer, the animal experiment (test) of…
CAS 1456994-27-6
NMDAR/TRPM4 inhibitor 9 (Compound 9) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.
CAS 163042-96-4
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
CAS 273727-89-2
ZM39923 is a potent, selective JAK3 inhibitor with pIC50 of 7.1, also potently inhibits human tissue transglutaminase (TGM2) with IC50 of 10 nM; ZM39923 is less potent for EGFR, JAK1 and CDK4 with pIC50 of 5.6, 4.4 and < 5.0, no activity fgor JAK2; alteres…
CAS 883031-03-6
HC-067047 is a potent and selective TRPV4 antagonist with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse TRPV4.
CAS 147084-10-4
For the detailed information of Alcaftadine, the solubility of Alcaftadine in water, the solubility of Alcaftadine in DMSO, the solubility of Alcaftadine in PBS buffer, the animal experiment（test） (test) of Alcaftadine, the cell expriment (test) of…
CAS 205754-33-2
8-hydroxy Efavirenz is a major oxidative metabolite of the non-nucleoside reverse transcriptase inhibitor efavirenz.8-hydroxy Efavirenz is formed when efavirenz is metabolized by the cytochrome P450 (CYP) isoform CYP2B6. It induces apoptosis in rat primary…
CAS 40054-69-1
Etizolam is a benzodiazepine analog. The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring, making the drug a thienodiazepine. It possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative…
CAS 1101854-58-3
JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.IC50 value: 8 nM [1]Target: MAGL inhibitorin vitro: JZL184 prolongs DSE in Purkinje neurons in cerebellar…
CAS 138847-85-5
PRE-084 hydrochloride is a high affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively).
CAS 375815-87-5
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a…
CAS 1079043-55-2
Deudextromethorphan (AVP-786) is a deuterated form of dextromethorphan/quinidine (AVP-923, Nuedexta). Deudextromethorphan, a glutamate-targeting agent, is an orally active N-methyl-D-aspartate (NMDA) receptor antagonist. Deudextromethorphan can be used for…
CAS 863918-78-9
Methoxy-X04 is a fluorescent dye that crosses the blood-brain barrier and selectively binds to beta-pleated sheets found in dense core amyloid Aβ plaques.
CAS 16590-41-3
A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively; also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for…
CAS 911115-16-7
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].
CAS 249889-64-3
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. IC50 value: 7.2 (pKb) Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses…
CAS 680590-49-2
EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively[1].
CAS 630117-19-0
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
CAS 467458-02-2
Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.…
CAS 1627091-47-7
MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.
CAS 850173-95-4
ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. IC50 value: 0.8 nM(Ki)Target: δ-opioid receptorADL-5859 (ADL5859) is an δ-opioid receptor agonist (Ki=0.84…
CAS 118476-85-0
DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) is a potent μ-opioid peptide agonist, affecting various patterns of locomotor activities.
CAS 875927-64-3
UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6; displays excellent wide selectivity against a wide range of other ion channels (including hERG, NMDA, and kainate channels), enzymes, and GPCRs;…
CAS 170846-89-6
E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
CAS 891016-02-7
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
CAS 191217-81-9
Pramipexole dihydrochloride hydrate is a selective dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research…
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
CAS 709676-56-2
TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and…
CAS 2097826-24-7
Yhhu-3792 is a novel small molecule that enhances the self-renewal capability of neural stem cells (NSCs) in vitro and in vivo via activating the Notch signaling pathway; activates Notch signaling pathway and promotes the expression of Notch target genes,…
CAS 83881-52-1
Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.Cetirizine crosses the blood-brain barrier…
CAS 1646499-97-9
ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay; displays >100-fold selectivity versus MrgX2; enhances the ability of BAM8-22 to inhibit…
CAS 2377379-39-8
BUN79398(MRGPRX1 agonist 1) is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect[1].
CAS 2562346-14-7
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in…
CAS 139180-30-6
ZM 241385 is a selective and high affinity A2A adenosine receptor antagonist.
CAS 174689-39-5
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
CAS 24211-36-7
AnCoA4 (AnCoA-4, AnCoA 4) is a potent Orai1 channel inhibitor that inhibits store-operated calcium (SOC) with EC50 of 0.88 uM; binds to the C terminus of Orai1, directly inhibits calcium influx through the channel and also reduces binding of STIM1; decreased…
CAS 152657-84-6
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential…
CAS 99755-59-6
A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with…
CAS 1610802-47-5
LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members; demonstrates fully protective against pentylenetetrazole-induced…
CAS 33507-63-0
Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Sequence: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
CAS 667427-75-0
TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6…
