N-0861 racemate is the racemate of N-0861. N-0861 is a selective adenosine A1 receptor antagonist.
MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].
Xelaglifam is a potent GPR40 agonist. Antihyperglycaemic activity[1].
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
Bromchlorbuterol hydrochloride is an active β-adrenergic agonist (β-agonist) and can be used for the research of pulmonary disease and asthma[1].
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit[1][2].
TGR5 agonist 3 (compound 8), a Cholic acid derivative, is a selective TGR5 agonist with an EC50 of 5 μM[1].
GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression.
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease[1][2].
[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist[1].
Riminkefon is a kappa opioid receptor agonist[1].
Cholera toxin is a multifunctional protein produced by Vibrio cholera. Cholera toxin is not just another enterotoxin that causes cholera but also able to influence the immune system in many ways.
Small Cardioactive Peptide B (SCPB), a neurally active peptide, stimulates adenylate cyclase activity in particulate fractions of both heart and gill tissues with EC50s of 0.1 and 1.0 μM, respectively.
Prednisolone is a glucocorticoid with the general properties of the corticosteroids.Target: Glucocorticoid ReceptorPrednisolone is a glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. Prednisolone, 5 or 50 mg/kg, was administered intravenously to adrenalectomized rats. Total plasma, free plasma, CBG-free plasma, and liver prednisolone concentrations were measured simultaneously with free hepatic cytosolic glucocorticoid receptor concentrations and tyrosine aminotransferase (TAT) activity of the liver as a function of time. prednisolone pharmacokinetics were dose-dependent, parameters describing receptor kinetics and TAT activity were constant at each prednisolone dose. The major determinants of receptor-mediated glucocorticoid activity are confirmed to be the availability of the receptor, drug-receptor dissociation rate, and corticosteroid persistence in the biophase [1, 2].
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
Montelukast is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
TH-Z816 is a reversible inhibitor againstKRAS(G12D)mutation with an IC50 value of 14 μM, which can be used in cancer research[1].
Desmethyl cariprazine is an active metabolite of Cariprazine[1]. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM)[2].
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P[1].
Tropanserin is a serotoninergic active compound, as well as a 5HT3 receptor antagonist. Tropanserin modulates Cardio-respiratory reflex effects of an exogenous serotonin challenge[1].
ONC206 is an analogue of TRAIL inducer ONC201[1]. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity[2].
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
KY1022 is a ras destabilizer. KY1022 targets the Wnt/ß-catenin pathway and inhibits development of metastatic colorectal cancer.
LH-RH (4-10) is a heptapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (4-10) produced in macrophages and type II pneumocytes[1].
ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor[1].
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibitingTGR5[1].
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease[1][2].
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).