BDW-OH is an active metabolite of BDW568. 2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc can be utilized in AUTAC synthesis.

2'2'-cGAMP, a synthetic CDN, binds STING in the immune response, inducing IFN-β. 2'2'-cGAMP binds weaker binding to STING than 2'3'-cGAMP. Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model.

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain.

ADP-β-S (trisodium) is an ADP analog and partial agonist. ADP-β-S (trisodium) induces human platelet aggregation and inhibits PGE1-stimulated adenylate cyclase.

LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine) with PD1/PDL1 blocker (BMS-1) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6)) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly.

Lon-TK is a glycolysis inhibitor + linker conjugate of LTB. LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research.

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity.

AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

VEN-02XX is an orally active and brain-permeable NLRP3 inhibitor. VEN-02XX inhibits the release of IL-1β and IL-18 (IC50 0.3 and 0.28 μM, respectively). VEN-02XX restores memory and cognition, inhibits microgliosis, and reduces neuroinflammation and tau pathology in the 5XFAD/Rubicon KO mouse model. VEN-02XX may be used in the study of Alzheimer's disease (AD).

NP3-253 is an NLRP3 inhibitor with oral activity and blood-brain barrier permeability, and NP3-253 can serve as a tool to further investigate the biological characteristics of NLRP3 in peripheral and neuroinflammatory model.

HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis.

Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib. 12-((4-Bromobutyl)amino)dodecanoic acid can be utilized in PROTAC synthesis.

Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib-induced mechanical hyperalgesia in rats. BI-113823 can be used for the research of chronic inflammatory pain.

Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib-stimulated cAMP production with an IC50 value of 18 nM. L-796778 acetate has anticonvulsant effect.

Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib that can be extracted from C. forskohlii. Deacetylforskolin activates rat adipocyte adenylyl cyclase (IC50 = 20 µM), inhibits glucose transport in rat adipocyte plasma membranes and exhibits antihypertensive activity.

Tarvicopan is an inhibitor for complement factor D.

Elsovaptan is the antagonist for vasopressin receptor that can be used in researchs of Alzheimer disease.

DM-4111, one of the major monohydroxyl metabolites of Tolvaptan. Obeticholic acid is a potent, selective and orally active FXR agonist.

A-49816 is an orally active diuretic that increases urine volume and sodium and chloride excretion. A-49816 at high doses (12.5, 15, and 20 mg) caused significant salt and chloride excretion and diuresis in experimental animals.

(R)-(+)-Tolvaptan ((R)-(+)-OPC-41061) is the (R)-(+) enantiomer of Tolvaptan.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research.

N-Methylphenethylamine (NMPEA) hydrochloride is a potent TAAR1 agonist. N-Methylphenethylamine hydrochloride also is a trace amine neuromodulator.

MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer.

SSTR4 agonist-1 (Compound 47) is a selective agonist for somatostatin receptor subtype 4 (SSTR4) with an EC50 of 4.7 nM. SSTR4 agonist-1 reveals a half-life > 130 minutes in human liver microsomes.

L-796778 acetate is a selective agonist of the sst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 acetate is a partial agonist that inhibits Forskolin

BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research.

SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.

Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).

Igmesine hydrochloride (JO 1784) is an orally active σ-receptor ligand capable of blocking the increase in colonic electromechanical activity induced by emotional stress. Igmesine hydrochloride also eliminates the colonic motility stimulation induced by dopamine, as well as the stimulation induced by centrally injected D1 or D2 receptor agonists. Furthermore, Igmesine hydrochloride can block the colonic motility responses induced by corticotropin-releasing factor (CRF) and ES through central cholecystokinin (CCK) release and/or activation of supraspinal CCK pathways.

CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively.