Product apis-gpcr-g-protein

Home > products > apis> gpcr-g-protein

Catalog	name	Description	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-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-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-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-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-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>

...

163