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R-C-1207 AZD2461 CAS:1174043-16-3 AZD-2461 is a potent PARP inhibitor,with IC50s of 5 nM,2 nM and 200 nM for PARP1,PARP2 and PARP3,respectively. price>
R-R-2907 ML221 CAS No.877636-42-5 ML221/CAS No.877636-42-5 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. price>
R-C-1208 Epacadostat (INCB 024360) CAS:1204669-58-8 Epacadostat(INCB 024360)is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1)inhibitor with an IC50 of 71.8 nM. price>
R-R-2908 Abaloparatide TFA Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis. price>
R-C-1209 IWR-1-endo CAS:1127442-82-3 IWR-1-endo(endo-IWR 1)is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A,induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. price>
R-R-2909 ML339 CAS No.2579689-83-9 ML339/CAS No.2579689-83-9 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 has no inhibitory effect on CXCR5,CXCR4,CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research. price>
R-C-1210 Marimastat CAS:154039-60-8 Marimastat(BB2516)is a broad spectrum and orally bioavailable inhibitor of MMPs,with potent activity against MMP-9(IC50=3nM),MMP-1(IC50=5nM),MMP-2 (IC50=6nM),MMP-14(IC50=9nM)and MMP-7(IC50=13 nM),used in the treatment of cancer.Marimastat(BB2516)is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels.As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes. price>
R-R-2910 Elabela(19-32) TFA Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart. price>
R-C-1211 SU-5614 CAS:1055412-47-9 SU5614 is a potent and selective FLT3 inhibitor.SU5614 reverts the antiapoptotic and pro-proliferative activity of FLT3 ligand(FL)in FL-dependent cells. price>
R-R-2911 TRV-120027 TFA TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment. price>
R-C-1212 oltipraz CAS:64224-21-1 Oltipraz has an inhibitory effect on HIF-1αactivation in a time-dependent manner,completely abrogating HIF-1αinduction at≥10μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM.Oltipraz is a potent Nrf2 activator. price>
R-R-2912 UNC9994 hydrochloride CAS No.2108826-33-9 UNC9994 hydrochloride/CAS No.2108826-33-9 is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity. price>
R-C-1213 S1RA CAS:878141-96-9 S1RA(E-52862)is a potent and selective sigma-1 receptor(σ1R,Ki=17nM) antagonist,showed good selectivity against σ2R(Ki>1000 nM). price>
R-R-2913 TRV-120027 CAS No.1234510-46-3 TRV120027/CAS No.1234510-46-3, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment. price>
R-C-1214 Balicatib(AAE-581) CAS No. 354813-19-7 Balicatib(AAE-581)is a potent and selective inhibitor of cathepsin K;10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B,L,and S. price>
R-R-2914 (Rac)-Tavapadon CAS No.1643462-64-9 (Rac)-Tavapadon ((Rac)-PF-06649751)/CAS No.1643462-64-9 is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity. price>
R-C-1215 Inauhzin(INZ) CAS:309271-94-1 Inauhzin is a potent SIRT inhibitor,which effectively reactivates p53 by inhibiting SIRT1 activity,promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. price>
R-R-2915 7-Fluorotryptamine hydrochloride CAS No.159730-09-3 7-Fluorotryptamine hydrochloride/CAS No.159730-09-3 is a potent agonist of GPRC5A. 7-Fluorotryptamine hydrochloride induces GPRC5A-mediated β-arrestin recruitment. 7-Fluorotryptamine hydrochloride can be used for research of immune and cancer signaling. price>
R-C-1216 Walrycin B CAS:878419-78-4 Walrycin B is a potent WalR inhibitor.The WalK/WalR(YycG/YycF)two-component system,which is essential for cell viability,is highly conserved and specific to low-GC percentage of Gram-positive bacteria,making it an attractive target for novel antimicrobial compounds. price>
R-R-2916 CCX-777 CAS No.1226686-36-7 CCX-777/CAS No.1226686-36-7 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3). price>