(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability[1][2].
CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections[1][2].
Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis[1].
S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.
MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research[1].
SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM[1].
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control[1].
Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations[1][3][4][5].
Methdilazine is an orally active antibiotic (histamine antagonist). Methdilazine can inhibit various mycobacterium with MIC values at 5-15 μg/mL in vitro and in vivo, which can be used for the research of infectious diseases[1][2].
Brexpiprazole D8 (OPC-34712 D8) is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).IC50 value: 1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1]Target: BRS-3in vitro: MK-5046 is a novel BRS-3 agonist, with improved BRS-3 potency, specificity, and pharmacokinetic properties that allows in-depth investigation of BRS3 agonism in preclinical species and is also potentially suitable for use in humans. MK-5046 exhibits no appreciable binding activity at the neuromedin B and gastrin-releasing peptide receptors, as well as many other receptors, ion channels, and enzymes. In a cell-based Ca2+ mobilization functional assay, MK-5046 activates human BRS-3 with similar agonist efficacy as the peptide BRS-3 agonist.[1] MK-5046 is a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity.[2]in vivo: MK-5046 is the first BRS-3 agonist with properties suitable for use in larger mammals. In dogs, MK-5046 treatment produced statistically significant and persistent weight loss, which was initially accompanied by increases in body temperature and heart rate that abated with continued dosing. MK-5046 also effectively reduced body weight in rats and caused modest increases in body temperature, heart rate, and blood pressure. MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity.[1]
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist[1].
Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases[1].
Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid[1].
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor[2].
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].
COR170 (11u) is a selective CB2 inverse-agonist which is a 4-quinolone-3-carboxylic acid derivative with a Ki value of 3.8 nM for CB2 receptor. COR170 can be used for the research of inflammation and neuroprotection[1][2][3].
Indusatumab (5F9 Monoclonal antibody) is an anti-human GUCY2C (Guanylate cyclase 2C) monoclonal antibody[1].
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder[1][2][3][4].
ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM[1].