Azathioprine (BW 57-322) sodium is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis[1][3].
Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain. Pain Phase 2 Clinical
Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.
L-m-Tyrosine is an unnatural amino acid, that has potential in the research of Parkinsons disease, Alzheimers disease, and arthritis[1].
Cassiaside is a naphthopyrone glucoside, shows mixed-type inhibition against BACE1 (IC50=4.45 μM; Ki=9.85 μM). Cassiaside possesses potential anti- Alzheimer's disease (AD) activity[1].
2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM[1][2].
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects[1].
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
RS 8359 is a selective and reversible MAO-A inhibitor, with antidepressant activity.
VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. VU 6008667 has high CNS penetration[1].
AVex-73 hydrochloride is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
Lanosterol-d6 is deuterium labeled Lanosterol. Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol s
DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively[1][2][3].
Etamivan is a respiratory stimulant drug, mainly used in the treatment of barbiturate overdose and chronic obstructive pulmonary disease.
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].
NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors[1][2].
RuBi-4AP, a derivative of 4-aminopyridine (4AP; HY-B0604), is a caged Kv channel blocker. RuBi-4AP contains a photolabile protecting group, allowing its effect to be controlled precisely in both space and time with light. RuBi-4AP can be used for the research of neuronal excitability, synaptic transmission, and signal propagation[1][2].
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1].
SKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase, but not PLC. SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia[1][2].
Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an acaricide[1].
α-Synuclein (67-78) (human) is the 67-78 fragment of α-Synuclein. α-Synuclein (67-78) (human) promotes network activity drive and blocks KCl-induced syt1L-ab uptake[1].
Adrenaline sulfate is a orally active hormone secreted by the medulla of the adrenal glands. Adrenaline sulfate is an α-adrenergic and β-adrenergic receptor agonist. Adrenaline sulfate can be used in the treatment of anaphylaxis. Adrenaline sulfate has the potential for the research of cardiac arrest[1][2][3][4].
RP 48497, an impurity of Eszopiclone, is a photodegradation product of Eszopiclone. Eszopiclone is a non-benzodiazepine sedative-hypnotic used in the treatment of insomnia[1].
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
AM-6538 (AM6538) is a potent, selective cannabinoid receptor CB1 antagonist with Ki of 5.1 nM.
PZ-1190 is a multitarget ligand for serotonin and dopamine receptors with potential antipsychotic activity in rodents[1].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells[1][2][3].
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects[1][2][3][4][5].
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease[1][2].