BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) [1].
A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors; induces dose-dependent cell death in SK-N-SH cells with EC50 of 7.6 uM, also demonstrates selective cytotoxic activity against PANC-1 pancreatic and MCF-7 breast cancer cell lines, with no significant effect on normal cells.
Akuammigine is an alkaloid that can be found in hook-bearing branch of Uncariarhynchophylla. Akuammigine is a is a very weak antagonist at pre- and postsynaptic α-adrenoceptor of the rat vas deferens[1][2].
L-Glutamine is a non-essential amino acid present abundantly throughout the body and is involved in gastrointestinal disorders.Target: mGluRGlutamine (abbreviated as Gln or Q) is one of the 20 amino acids encoded by the standard genetic code. It is not recognized as an essential amino acid, but may become conditionally essential in certain situations, including intensive athletic training or certain gastrointestinal disorders. Its side-chain is an amide formed by replacing the side-chain hydroxyl of glutamic acid with an amine functional group, making it the amide of glutamic acid. Its codons are CAA and CAG. In human blood, glutamine is the most abundant free amino acid, with a concentration of about 500-900 μmol/L. Glutamine is synthesized by the enzyme glutamine synthetase from glutamate and ammonia. The most relevant glutamine-producing tissue is the muscle mass, accounting for about 90% of all glutamine synthesized. Glutamine is also released, in small amounts, by the lung and the brain. Although the liver is capable of relevant glutamine synthesis, its role in glutamine metabolism is more regulatory than producing, since the liver takes up large amounts of glutamine derived from the gut. The most eager consumers of glutamine are the cells of intestines, the kidney cells for the acid-base balance, activated immune cells, and manycancer cells. In respect to the last point mentioned, different glutamine analogues, such as DON, Azaserine or Acivicin, are tested as anticancer drugs.
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist tifluadom[1].
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.Target: Glucocorticoid ReceptorFluocinonide is a potent glucocorticoid steroid used topically as an anti-inflammatory agent for the treatment of skin disorders such as eczema and seborrhoeic dermatitis. Fluocinonide ranks as a "high-potency" topical corticosteroid. Minimal amounts should be used for a minimal length of time to avoid the occurrence of adverse effects. Fluocinonide should not be used if infection is present. Fluocinonide is used in veterinary medicine. It is a treatment for allergies in dogs. Natural systemic cortisol concentrations can be suppressed for weeks after one week of topical exposure. From Wikipedia.
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].
Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity[1][2][5].
4'-O-Methylnyasol is an inhibitor of β-hexosaminidase. 4'-O-Methylnyasol inhibits β-hexosaminidase release from rat basophilic leukemia-2H3 cells with an IC50 of 52.67 μM[1].
Potent, allosteric GPR55 antagonist
Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain[1].
Dexpramipexole 2Hcl(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist. IC50 Value:Target: Dopamine ReceptorDexpramipexole has been found to have neuroprotective effects and is being investigated for treatment of amyotrophic lateral sclerosis (ALS). Dexpramipexole reduces mitochondrial reactive oxygen species (ROS) production, inhibits the activation of apoptotic pathways, and increase cell survival in response to a variety of neurotoxins and β-amyloid neurotoxicity. Compared to the S-(-) isomer, Dexpramipexole has much lower dopamine agonist activity.
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
a-Helical Corticotropin Releasing Factor (12-41) is a 30 amino acids long, α-helical analogue of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH). a-Helical Corticotropin Releasing Factor (12-41) would suppress the stimulatory effect[1][2].
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model[1].
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 elicits deep and durable suppression on RAS pathway activity in KRASG12C tumor models[1].
Dapiprazole hydrochloride is a potent α-adrenergic blocking drug, which is used to reverse mydriasis after eye examination.(1) It inhibits amphetamine toxicity and alcohol and morphine withdrawal syndromes, produces sedation, blocks conditioned avoidance reflexes and reduces the response to noxious stimuli.(2) The orally administrated daily dose varied from 30 to 90 mg.
(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively). IC50 Value: 1.97 nM(Ki for β1); 2.0 nM(Ki for β2)Target: β-adrenergic receptor(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain barrier. Timolol maleate does appear to have some local anesthetic properties in human cornea after chronic use by susceptible individuals.
SUVN-G3031 (SUVN-G 3031) is a potent, selective, orally active histamine H3 receptor (H3R) inverse agonist with Ki of 8.73 nM (hH3R); exhibited an IC50 of 20 nM with progressive inhibition of (R)-α-methylhistamine (0.03 µM) induced agonist activity in [35S]-GTPγS binding assay using CHO-K1 cells expressing human H3R membranes; reverses (R)-α-methylhistamine induced dipsogenia in vivo. Parkinson Disease Phase 1 Clinical
S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].
DPP-4/GPR119 modulator 2 (Compound 20i) is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist with an IC50 of 0.22 µM for DPP-IV and an EC50 of 0.95 µM for GPR119. DPP-4/GPR119 modulator 2 can be used for diabetes research[1].
Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to treat asthma.
MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
Prasugrel hydrochloride is a platelet inhibitor with IC50 value of 1.8 μM.Target: P2Y12 receptorPrasugrel hydrochloride is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI [2].Prasugrel hydrochloride reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel hydrochloride AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 Μm [2]. Clinical indications: Acute coronary syndrome; Ischemic heart disease; Sickle cell anemia; Stroke; Vascular occlusive diseaseFDA Approved Date: February 2009Toxicity: Hypertension; Headache; Hypercholesterolemia/hyperlipidemia; Nausea; Epistaxis
I-191 is a protease-activated receptor 2 (PAR-2) signaling pathway inhibitor extracted from patent WO2015048245A1. I-191 inhibits PAR-2 activators such as SLIGKV, Trypsin, and Thrombin with IC50s of 0.0014 μM, 0.0023 μM, 0.32 μM, respectively[1].
Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[1][2].
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].