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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>
R-C-1217 TPT-260 CAS NO. 769856-81-7 TPT-260(TPU260)is a thiophene thiourea derivative with molecule weight 260.00 in free base form;There is no formal name yet,we temporally call this molecule as TPT-260. price>
R-R-2917 ML192 CAS No.460331-61-7 ML192/CAS No.460331-61-7 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation. price>
R-C-1218 Altiratinib CAS:1345847-93-9 Altiratinib,also known as DCC-270,DP-5164,is an oral,selective and highly potent inhibitor of MET,TIE2,VEGFR2 and TRK kinases with potential anticancer activity.DCC-2701 effectively reduces tumor burden in vivo and blocks c-MET pTyr(1349)-mediated signaling,cell growth and migration as compared with a HGF antagonist in vitro. Importantly,DCC-2701 is anti-proliferative activity was dependent on c-MET activation induced by stromal human fibroblasts and to a lesser extent exogenous HGF. price>
R-R-2918 ELA-21 (human) CAS No.2245073-05-4 ELA-21 (human)/CAS No.2245073-05-4 is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways. price>
R-C-1219 CTX0294885 CAS:1439934-41-4 CTX-0294885 is a novel broad-spectrum kinase inhibitor.CTx-0294885 exhibits inhibitory activity against a broad range of kinases in vitro. price>
R-R-2919 GPR35 agonist 2 CAS No.494191-73-0 GPR35 agonist 2 (compound 11)/CAS No.494191-73-0 is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively. price>
R-C-1220 TH588 CAS:1609960-31-7 TH588 is a potent and selective MTH1(NUDT1)inhibitor with IC50 of 5 nM.It has no relevant inhibition of any of the other tested proteins at 100 μM,although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes,GPCRs,kinases,ion channels and transporters at 10 μM. price>