RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
RET-IN-18 is a pyridone compound. is a potent inhibitor of RET. RET-IN-18 is a potent inhibitor of RET. RET-IN-18 has the potential for the research of diseases related to irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as cancers, and neurodegenerative diseases (extracted from patent WO2022017524A1, compound 1)[1].
(S)-BAY 73-6691 is the inactive isomer of BAY 73-6691 (HY-104028), and can be used as an experimental control. BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor[1].
Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia.
Uperolein is a physalaemin-like endecapeptide, produced in the skin of Uperoleia rugosa and Uperoleia marmorata. Uperolein has a spasmodic effect on both the gastrointestinal tract and longitudinal muscles[1][2][3].
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research[2].
Pteryxin, a coumarin in Peucedanum japonicum Thunb leaves, exerts antiobesity activity[1]. Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor, with an IC50 of 12.96 μg/ml[2].
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat[1].
IPN-60090 dihydrochloride is an orally bioavailable and selective inhibitor of GLS1 (the kidney-type glutaminase), an important enzyme for metabolic energy production. IPN-60090 dihydrochloride can be used in the research of GLS1-mediated diseases[1][2].
Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity[1][2][3].
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders[1].
Acamprosate is an orally active prototypic neuromodulator. Acamprosate can be used for the research of alcohol dependence and alcoholism[1].
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases[1][2].
MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.Target: Potassium ChannelDoxapram is a respiratory stimulant. Doxapram (15-150 microM) also evoked 3H overflow in a concentration dependent manner, and doxapram-evoked release was inhibited by the Ca2+ channel blocker nifedipine (5 microM). Analysis of released tritiated compounds suggested that doxapram preferentially stimulated the release of dopamine. Our results indicate that the mechanism of action of doxapram shares similarities with that of hypoxia in the carotid body [1]. Doxapram (1-100 microM) caused rapid, reversible and dose-dependent inhibitions of K+ currents recorded in type I cells (IC50 approximately 13 microM). doxapram was also seen to directly inhibit Ca(2+)-independent K+ currents. Doxapram was a more potent inhibitor of the Ca(2+)-activated K+ currents recorded under control conditions. Doxapram (10 microM) was without effect on L-type Ca2+ channel currents recorded under conditions where K+ channel activity was minimized and was also without significant effect on K+ currents recorded in the neuronal cell line NG-108 15, suggesting a selective effect on carotid body type I cells. The effects of doxapram on type I cells show similarities to those of the physiological stimuli of the carotid body, suggesting that doxapram may share a similar mechanism of action in stimulating the intact organ [2].
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities[1][2].
Ipalbidine is an alkaloid extracted from ipomoea Hardwickki Hemsl. Ipalbidine has dose-dependent analgesic effects[1].
4-Butyl-alpha-agarofuran (AF 5) is an anxiolytic and antidepressant agent. 4-Butyl-alpha-agarofuran a α-agarofuran derivative that can be isolated from Gharu-wood. 4-Butyl-alpha-agarofuran can be used for the research of neurological disease research[1].
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth[1].
α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC50 value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC50= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development[1].
Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
EHT 1864 is a small molecule inhibitor of Rac1 signaling; modulate γ-Secretase-mediated APP processing.IC50 value:Target: Rac1 inhibitorin vitro: EHT 1864 blocks Aβ 40 and Aβ 42 production but does not impact sAPPα levels and does not inhibit γ-secretase. Rather, EHT 1864 modulates APP processing at the level of γ-secretase to prevent Aβ40 and Aβ42 generation. This effect does not result from a direct inhibition of the γ-secretase activity and is specific for APP cleavage, since EHT 1864 does not affect Notch cleavage [1]. EHT 1864 specifically inhibited Rac1-dependent platelet-derived growth factor-induced lamellipodia formation. Furthermore, our biochemical analyses with recombinant Rac proteins found that EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms, and this association promoted the loss of bound nucleotide, inhibiting both guanine nucleotide association and Tiam1 Rac guanine nucleotide exchange factor-stimulated exchange factor activity in vitro [2].in vivo: EHT1864 significantly reduces Aβ 40 and Aβ 42 levels in guinea pig brains at a threshold that is compatible with delaying plaque accumulation and/or clearing the existing plaque in brain [1].
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases [1].
Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines[1].
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats[1][2].
4'-Hydroxy diclofenac D4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease[1].
Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
[pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM[1].
Methylfurmethide is an acetylcholine receptor. Methylfurmethide blocks the uptake of atropine. Methylfurmethide can be used to study the properties of acetylcholine receptors in intestinal smooth muscle [1].