Renin IN-2 (compound 27) is a human renin inhibitor with an IC50 of 0.059 μM. Renin IN-2 exhibits oral efficacy. Renin IN-2 can be used in the research of hypertension.

rel-ML123 is a negative control probe of ML123 (trans-Racemate).

RdRP-IN-10 is a SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor with an IC50 value of 5.78 μM. RdRP-IN-10 forms covalent binds with SARS-CoV-2 nsp8 Cys114, disrupts nsp8-nsp12 stabilizing interactions. RdRP-IN-10 inhibits SARS-CoV-2 RdRp-mediated RNA polymerization without interfering with RNA-RdRp complex binding. RdRP-IN-10 exerts antiviral effects in cellular models. RdRP-IN-10 can be used for the research of SARS-CoV-2 infection.

RBP4-IN-3 (Compound 38) is a retinol-binding protein 4 (RBP4) inhibitor. RBP4-IN-3 can be used in studies related to cardiovascular diseases and obesity.

RB-105 is an inhibitor of angiotensin-converting enzyme (ACE) (Ki = 4.2 nM) and neutral endopeptidase (NEP) (Ki = 1.7 nM). RB-105 after inhibiting ACE reduces the production of Ang II and increase the level of bradykinin. RB-105 after inhibiting NEP increases the level of natriuretic peptide and further increases the level of bradykinin, thereby generating a powerful synergistic effect. RB-105 has significant antihypertensive and natriuretic effects in both spontaneously hypertensive rats and normal blood pressure rats. RB-105 can be used for research on hypertension.

Rapamycin-butyl ester (Sirolimus-butyl ester) (Compound 9) is a derivative of Rapamycin. Rapamycin-butyl ester exhibits antiproliferative effects against liver cancer cells and renal cancer cells. Rapamycin-butyl ester can be used in research related to liver cancer and renal cancer.

RANKL-IN-2 is an orally active RANKL inhibitor with Kd values of 3.21 μM and 4.625 μM in the SPR and MST assays, respectively. RANKL-IN-2 binds to RANKL to interfere with RANKL-RANK interaction. RANKL-IN-2 suppresses osteoclastogenesis by inhibiting ROS, MAPK and NF-κB pathways. RANKL-IN-2 inhibits osteoclastogenesis via inhibition of RANKL-induced osteoclast formation, bone resorption, and osteoclast-specific gene and protein expressions in vitro.RANKL-IN-2 prevents bone loss in ovariectomized osteoporosis mice.RANKL-IN-2 can be used for the research of osteoporosis.

Ramiprilat acyl-β-D-glucuronide is an acyl glucuronide metabolite of Ramiprilat. Ramiprilat acyl-β-D-glucuronide undergoes methylation on its glucuronic acid moiety during solid phase extraction with strong cation exchanger cartridges, forming a methylated derivative. Ramiprilat acyl-β-D-glucuronide undergoes in-source conversion to Ramiprilat in mass spectrometry, with conversion extent proportional to declustering potential voltage.

RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis.

RAFKBP12 is a FKBP12 PROTAC degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination. (Pink: FKBP12 ligand ; Blue: RPN13 ligand ; Black: linker).

RA190-PEG1-NH2, RA190 derivative, is an E3 ligase ligand. RA190-PEG1-NH2 can be used to synthesis FKBP12 PROTAC degrader RAFKBP12.

R214127 is a selective mGlu1 receptor antagonist with IC50 values of 6 and 14 nM for rat and human mGlu1a. R214127 acts on a site from the glutamate binding pocket, and competes for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists.

R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression.\nR-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis.

R06039-696 is a neuropeptide S receptor (NPSR) agonist with an EC50 of 91 nM. R06039-696 can participate in regulating various biological functions such as arousal, stress and anxiety responses, memory processes, and food intake by activating NPSR.

R06039-636 is an agonist of the Neuropeptide S receptor (NPSR) with an EC50 value of 94nM.

Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research.

Quindoxin is an antibacterial and growth promoter, commonly used in the livestock industry. Quindoxin exhibits clear dose-dependent mutagenic activity against Salmonella typhimurium TA98 and TA100 strains. Quindoxin can cause DNA damage and has potential genotoxicity and carcinogenic risks.

QS-IN-1 (Compound 10 in Table 2 on page 18) is a quorum sensing (QS) inhibitor with an IC50 of 1.22 μM against agr-type QS. QS-IN-1 is applicable to the research of bacterial infections.

PZ-1129 is a selective 5-HT7 receptor ligand with a Ki of 7 nM. PZ-1129 shows Ki values of 159 and 24 nM for 5-HT1A receptor and D2 receptor. PZ-1129 can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 13.7 nM). PZ-1129 can be used for the research of emotional disorders, such as depression and bipolar disorder.

Pyridine-3-sulfonyl chloride belongs to the substituted sulfonyl chloride class. Due to its high proton affinity, it can be used as a derivatizing agent.

PXS 64, a mannose-6-phosphate (M6P) analogue. a lipophilic prodrug of PXS 25. PXS 64 is an effective anti-fibrotic agent by inhibiting the activation of latent TGF-β1. PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. PXS 64 reduces TGFβ-mediated collagen IV, fibronectin, MCP-1, and phospho-smad2 expression in kidney cells. PXS 64 reduces collagen deposition in dermal scar fibroblasts. PXS 64 can be used for the research of chronic kidney disease, idiopathic pulmonary fibrosis, scarring.

PXS 25 is a cation-independent mannose 6-phosphate receptor (CI-M6PR) inhibitor that inhibits CI-M6PR-mediated activation of latent TGF-β1. PXS 25 inhibits conversion of high glucose-induced latent TGF-β1 to active TGF-β1 in proximal tubule cells under normoxic conditions. PXS 25 suppresses high glucose-induced fibronectin, collagen IV production, and phosphorylated Smad 2 in proximal tubule cells under normoxic conditions. PXS 25 has antifibrotic properties in skin fibroblasts. PXS 25 can be used for the research of diabetic nephropathy.

PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.

PTPN2-IN-3 (example 52) is a PTPN2 inhibitor that can be used in tumor research.

PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma.

p-Toluenesulfonamide-15N is the 15N-labeled p-Toluenesulfonamide. p-Toluenesulfonamide is an intermediate and plasticizer. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum.

PTH1R agonist 4 (Example 63) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC50 value greater than 7. PTH1R agonist 4 can be used for the study of bone diseases, such as osteoporosis.

PTH1R agonist 1 (Example 2) is a parathyroid hormone 1 receptor (PTH1R) agonist. PTH1R agonist 1 can be used for research of hypoparathyroidism and osteoporosis.

PTERi is a selective inhibitor of PTER with selectivity towards HDACs. PTERi increases the level of N-acetyltaurine in both lean and obese mice, and reduces food intake in obese mice. PTERi can be used in the research of obesity.

PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.