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.

Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness.

Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.

HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute treatment of migraine.

Vicasinabin is the potent agonist of cannabinoid receptor 2 (CB2). Vicasinabin has the potential for the research of human diseases including chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and other related diseases (extracted from patent US20130116236A1).

Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family.

Mopivabil is the antagonist of angiotensin II receptor.

Mepixetil is a potent antagonist of angiotensin II receptor.

Azilsartan mopivabil is the potent antagonist of angiotensin II receptor.

Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A).

KUC-7322, a selective β3 -adrenoceptor agonist, is the active form of ritobegron. Ritobegron decreases intravesical pressure with minimal effects on the cardiovascular system.