ML375 (VU-0483253) is a potent, highly selective M5 NAM with submicromolar potency (human M5 IC50=300 nM, rat M5 IC50=790 nM, M1-M4 IC50> 30 uM), exhibts excellent multispecies PK, high CNS penetration, and enantiospecific inhibition.
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively.
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
(D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist[1].
[8-L-arginine] deaminovasopressin (dAVP) is a vasopressin analog[1].
LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats., and displays efficacy as a feeding inhibitor[1].
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].
Septide ((Pyr6,Pro9)-Substance P) is a potent NK1 receptor agonist with a Kd value of 0.55 nM[1].
BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) . 1) Reduces ischemia-induced ventricular arrhythmias in a rat model.2) BQ-123 prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.3) The reference for animal injections is 6.7 mg/kg. 4) BQ-123 decreased IL-1β and TNFα in the placenta while also decreasing transcription of ET-1 in the uterus.
CCR2 antagonist 3 is a chemokine receptor 2 (CCR2) antagonist.
Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM.
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].
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].
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.
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.
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.
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