(Rac)-Levomepromazine-d3 ((Rac)-Methotrimeprazine-d3) hydrochloride is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility[1].
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
Cinacalcet hydrochloride is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Homatropine Bromide is muscarinic AChR antagonist that is an anticholinergic medication.Target: mAChRHomatropine is an anticholinergic medication that is an antagonist at muscarinic acetylcholine receptors and thus the parasympathetic nervous system. Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs [1]. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses [2]. Homatropine [14C]methylbromide administrated rectal achieves higher and rapid peak plasma concentrations than by the other routes in rats whether HMB-14C is administered in a water-soluble suppository base or in aqueous solution, retained 28% of the 14C has been excreted in the urine while 56% remained in the large intestine after 12 hours. Unlabelled Homatropine methylbromide, given in rectal suppositories to anaesthetized rats, causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure [3].
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4[1].
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an opioid-receptor antagonist[1].
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A[1].
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells[1][2].
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model[1].
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner[1].
GGTI-286 is a CAAX peptidomimetic that is a potent, cell-permeable, and selective inhibitor of GGTase I with IC50 of 2 uM, 25-fold more potent than FTI-277; inhibits processing of the geranylgeranylated protein Rap1A; inhibits oncogenic K-Ras4B stimulation with IC50 of 1 uM; reduces nuclear localization of β-catenin and transcription dependent on β-catenin/T cell factor in mammalian cells; has significant antiproliferative effect in human malignant glioma cells.
Strontium ranelate(S12911) stimulates the calcium sensing receptors (CaSR) and leads to the differentiation of pre-osteoblast to osteoblast which increases the bone formation.IC50 value:Target: CaSRStrontium Ranelate is a bone metabolism modulator that inhibits bone resorption while maintaining bone formation. Strontium Ranelate acts by increasing bone formation and decreasing bone resorption, thus rebalancing bone turnover in favour of bone formation, an effect that results in increased bone mass and strength. Commonly used as an antiosteoporotic. Strontium Ranelate has shown efficacy in preventing early postmenopausal bone loss and reducing the risk of hip fracture in women with postmenopausal osteoporosis.
Dynorphin B (1-9) is a neuropeptide and N-terminal cleavage product of dynorphin B. The formation of dynorphin B (1-9) is blocked by N-ethylmaleimide (NEM), a non-selective inhibitor of cysteine peptidases[1].
Uridine 5'-diphosphate sodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine 5'-diphosphate sodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis[1][2].
Doxylamine D5 succinate is deuterium labeled Doxylamine, which is a first generation antihistamine.
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].
Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis. The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form. From Wikipedia.
L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors[1][2].
Carboprost tromethamine is the synthetic 15-methyl analogue of prostaglandin F2α. Carboprost tromethamine can effectively promote law contraction of the uterus and significantly reduce the amount of bleeding during and after delivery[1][2].
Teoprolol is a β-adrenergic receptor blocker.
Antiplatelet agent 1 (compound 7q) is a Ticagrelor analoguehas, possessing antiplatelet activity. Antiplatelet agent 1 can be used for researching platelet aggregation[1].
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity[1].
ACT-132577 is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
L-Glutamine-5-13C (L-Glutamic acid 5-amide-5-13C) is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia; significantly restores both scopolamine- and MK-801-induced cognitive dysfunction and demonstrates antipsychotic potential. Alzheimer Disease Phase 2 Clinical