Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect[1][2].
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
Methdilazine hydrochloride is an orally active antibiotic (histamine antagonist). Methdilazine hydrochloride 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].
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].
GSK1104252A is a potent and selective GPR119 agonist. GSK1104252A can be used for type 2 diabetes research[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].
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake[1].
Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria[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].
AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.
KRAS G12C inhibitor 46 (compound WX003) is a potent KRAS G12C inhibitor[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.
Lofexidine hydrochloride is an α2A-adrenergic receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.Target: β-2 Adrenergic ReceptorRitodrine is a tocolytic drug, used to stop premature labor. Ritodrine can significantly prolong a short interval more quickly but with relatively more side effects than magnesium sulphate. Stratified RCTs for different gestational ages and different labour stages should be designed for further study [1]. Ritodrine is a beta-2 adrenergic receptor agonist - a class of medication used for smooth muscle relaxation. Since ritodrine has a bulky N-substituent, it has high β2-selectivity. Also, the 4'-hydroxy on the benzene ring is important for activity as it is needed to form hydrogen bonds. However, the 4'-hydroxy makes it susceptible to metabolism by COMT. Since it is β2-selective it is used for premature labor [2].
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.
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour[1].
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].
Zicronapine (Lu 31-130) fumarate is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors[1][2].
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.
(±)-SLV319 is the racemate of SLV319. SLV319 is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.
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].
MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity[1][2][3].
BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.
GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain[1][2].
Niperotidine is a histamine H2-receptor antagonist.