Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells.

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit.

PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC50 = 61 nM; pS6, EC50 = 71 nM).

Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1).

JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM respectively).

TLR7/8 agonist 4 TFA (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity.

Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1).

Poly(I:C) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Poly(I:C) present in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA.

Polvitolimod is a TLR7 agonist for treatment of cancer and infectious disease.

GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines.

Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

SN-008, a less active SN-011 analog, can be used as a negative control.

ARB-272572 is a potent small-molecule PD-L1 inhibitor with an IC50 value of 400 pM.

PD-L1-IN-1 is a potent PD-L1 inhibitor with an IC50 of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells.

NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107).

L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is an endogenous bioactive sphingolipid. L-threo Lysosphingomyelin (d18:1) is a potent S1P receptor agonist with EC50s of 19.3, 131.8, and 313.3 nM for hS1P1, hS1P3, and hS1P2, respectively.

S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).

Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1).

Riminkefon is a kappa opioid receptor agonist.

Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.

Talaglumetad hydrochloride is a prodrug of thetype II metabotropic glutamate receptor (mGluR2/3) agonist Eglumegad for the treatment of anxiety.

Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo.

Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia.

Sabcomeline (hydrochloride) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition.

Milameline is a muscarinic receptor agonist that improves cognition.

MK-6884-11C is a positron emission tomography (PET) imaging agent for the study of M4 muscarinic receptor positive allosteric modulators (PAMs) in neurodegenerative diseases.

Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to treat asthma.

Ecnoglutide is a glucagon-like peptide 1 (GLP-1) receptor agonist.

Utreglutide is a potent glucagon-like peptide 1 (GLP-1) receptor agonit.

Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. Raclopride binds to D2 and D3 receptors with dissociation constants of between 1.8 nM and 3.5 nM, but has a very low affinity for D4 receptors.