RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.IC50 & Target: EC50: 0.77 μM (hTRPV4), 4.0 μM (mTRPV4), 4.1 μM (rTRPV4) .

Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases.IC50 & Target:NF-kappaB

Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[2].In Vitro: Isolated perfused heart preparations from guinea-pigs developed arrhythmic contractions following the administration of Ro 363 in doses producing 70-100% of its […]

Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM)[2].

RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10?μM at P2X1,2,4,5,7).IC50 & Target: pIC50: 5.9 (human homomultimeric P2X3 receptor); 7.0 (human […]

Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[2].In Vitro: Ro 24-7429 (0.1-5 μM; 3 days) induces apoptosis of cultured PBMCs in a dose-dependent manner.Ro 24-7429 (1-25 μM) also induces apoptosis and inhibits antigen-induced lymphocyte […]

RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects[2].IC50 & Target:EC50: 1 nM (Melanocortin 4 receptor (MC4R)), 8 nM (MC1R), 675 nM (MC3R) […]

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor […]

RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.In Vitro: RO5166017 showed high affinity and potent functional activity at mouse, rat, cynomolgus monkey, and human TAAR1 stably expressed in HEK293 cells as well as […]

RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric therapeutics.

RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines.RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system.RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern […]

RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect[2].In Vivo: RO5263397 (0.1-1.0?mg/kg; p.o.; dosing at the mid-light phase (ZT6)) increased wake time at 0.3 and 1?mg/kg[2].RO5263397 (0.3 and 1.0?mg/kg; p.o.) decreases […]

Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research[2].In Vitro: Robatumumab (0.02-80 nM; 0.5 or 4 h) downregulates IGF-IR and inhibits both basal and IGF-I-induced phosphorylation of IGF-IR and IRS-1 in SK-N-FI […]

Robinetin (3,3′,4′,5′,7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation[2].In Vitro: Robinetin (0.1-10 μM; 1 h) inhibits HIV integrase cleavage and integration in a dose-dependent manner.Robinetin inhibits the DNA synthesis in Proteus vulgaris, and the […]

Robinin is present in?flavonoid?fraction of?Vigna unguiculata?leaf. Robinin inhibits upregulated expression of TLR2 and TLR4. Robinin ameliorates oxidized low density lipoprotein?(Ox-LDL) induced inflammatory insult through TLR4/NF-κB pathway.

Rochelle potassium sodium tartrate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.IC50 & Target: Ki: 21.5 nM (EGFRL858R/T790M), 303.3 nM (EGFR)In Vitro: Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more […]

Roemerine, an aporphine alkaloid, isolated from the leaves of Fibraurea recisa Pierre, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.

Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors[2].

Roginolisib is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases.In Vitro: Roginolisib (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280?nM. Roginolisib inhibits B cell proliferation […]

Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease.

Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).IC50 & Target: Ki: 7.53 nM (5-HT2A), 8.19 nM (sigma-2)In Vitro: Roluperidone (CYR-101) also shows binding affinity for α1-adrenergic receptors but low or no affinity for […]

Romifidine hydrochloride is an α2 adrenergic receptor agonist. Romifidine hydrochloride shows sedation effects in vivo[2].In Vivo:Romifidine hydrochloride (80 μg/kg; i.v. once) produces sedative effects with significantly greater drooping during the 45-90 min time period in welsh mountain ponies.Romifidine hydrochloride (40, 80 and 120 mg/kg; i.v. at seven-day intervals) shows a shallower and shorter-lived sedation than […]

Romosozumab is a humanized monoclonal anti-sclerostin antibody, it promotes bone formation and inhibits bone resorption by inhibiting sclerostin. Romosozumab can be used for the research of osteoporosis[2].In Vivo:Romosozumab (30 mg/kg; s.c. twice a week for 10 weeks) converts trabecular rods into trabecular plates in cynomolgus monkeys.Romosozumab (3 and 30 mg/kg; s.c. once a week for […]

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.In Vitro: RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3?μM in Th17 cell differentiation assay.In Vivo: RORγt inverse agonist 13 (Compound 3i, 25 […]

RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.IC50 & Target: EC50: 0.22 μM (hRORγ), 0.15 μM (RORγt, human IL-17 cells)

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.In Vivo: RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model.RORγt Inverse agonist 6 […]

Rose Bengal sodium, a synthetic fluorescein derivative, and is a crimson-coloured dye with the principal component being 4,5,6,7-tetrachloro-2,4,5,7-tetraiodo fluorescein. Rose Bengal sodium has been widely used as an ophthalmic diagnostic agents, and can detect desiccated or damaged cells on the ocular surface. Rose Bengal sodium exhibits antiviral activities[2].

Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.In Vitro: Roseoflavin, a chemical analog of flavin mononucleotide (FMN) and riboflavin that has antimicrobial activity, can directly bind to FMN riboswitch (Kd~100 nM) aptamers and downregulate the expression of an FMN riboswitch-lacZ reporter […]

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator with anticancer effects. Roslin 2 bromide binds FAK, disrupts the binding of FAK and p53.In Vitro: Roslin 2 bromide decreases cancer cell viability and clonogenicity in a p53-dependent manner. Roslin 2 bromide increases p53 transcriptional activity that is inhibited by FAK using p21, Mdm-2, and Bax-promoter […]

Rosopatamab (HJ 591) is a humanised anti-PSMA monoclonal antibody that can be used in cancer research, particularly in prostate cancer[2].IC50 & Target:PSMA[2].

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[2]. Rottlerin […]

Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.IC50 & Target:Hypoxia-inducible factor prolyl-hydroxylaseIn Vitro:Roxadustat (5-50 μM; 6 hours) significantly inhibits TBHP-induced apoptosis in PC12 cells[2].Roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression in PC12 cells[2].In Vivo:Roxadustat (50 mg/kg; […]

Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[2].IC50 & Target: Ki: 6.05 μM (PKA I) and 9.75 μM (PKA II)In Vitro: A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) […]

Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases[2].IC50 & Target: Ki: 6.05 μM (PKA I) and 9.75 μM (PKA II)In Vitro: A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) […]

RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.In Vitro: RP101988 is a substrate of P-gp and breast cancer resistance protein (BCRP) drug transporters[2].

RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.IC50 & Target: Topoisomerase type I; AChE

RR-RJW100, the enantiomer of RJW100, is an nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1) agonist. RJW100 can be synthesized as two enantiomers, RR-RJW100 and SS-RJW100, with RR-RJW100 shown to be the more potent LRH-1 agonist. RR-RJW100 is involved in the regulation of metabolic homeostasis and is used in studies of […]

RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.

RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats[2].In Vitro:RS-102221 hydrochloride (0.3-300nM; 24 h) promotes the differentiation of […]

RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis[2].In Vitro:RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells.RU-301 (10 μM; 24 h) […]

RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K+ channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).

Ru(dpp)3(PF6)2 is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.IC50 & Target:NF-κB

Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes[2].IC50 & Target:IC50:4.7 nM and 5.9 nM (PKCβ), Ki: 2 nM (PKCβ)sup>[1]In Vitro: Ruboxistaurin mesylate […]