Vercirnon is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes[1].
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role[1].
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinases MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC50 value of 95 nM.
Denufosol tetrasodium (INS37217) is a long-acting P2Y2 receptor agonist, which exhibits an EC50 of ~10 μM for P2Y2 receptor activation[1].
Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (Substance P (HY-P0201)). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect[1][2].
Arbutamine hydrochloride is a short-acting, potent and nonselective β-adrenoceptor agonist. Arbutamine hydrochloride stimulates cardiac β1-, tracheal β2-, and adiopocyte β3- adrenergic receptors. Arbutamine hydrochloride provides cardiac stress increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine hydrochloride can be used for cardiac stress agent [1][2][3].
ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion[1].
2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation[1][2][3].
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis[1].
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research[1][2].
KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2)[1].
Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.IC50 value: 32 uMTarget: H1-receptorLoratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.
Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist[1][2].
Ebastine-d5 (LAS-W 090-d5) is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].
Astemizole, a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has anticholinergic and antipruritic effects[1][2].
Desmopressin(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin. IC50 Value:Target: Vasopressin ReceptorThe antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.
GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats[1][2].
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors[1].
Retrobradykinin has the reverse sequence of Bradykinin (HY-P0206). Retrobradykinin has no significant kinin activity and can be used as a negative control for Bradykinin[1].
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].
Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
Goserelin(ICI 118630) is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).IC50 value:Target: GnRH agonistGoserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.
Nexinhib20 is a specific Rab27a-JFC1 interaction inhibitor with a calculated IC50 of 2.6 μM. Nexinhib20 significantly inhibits superoxide anion production. Nexinhib20 efficiently decreases exocytosis of azurophilic granules in neutrophils stimulated with fMLP, GM-CSF or both. Nexinhib20 has a significant anti-inflammatory activity[1].