Product apis-gpcr-g-protein

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Catalog	name	Description	price
R-R-2906	AC1-IN-1 CAS No.2762422-55-7	AC1-IN-1/CAS No.2762422-55-7 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC50 of 0.54 µM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity.	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-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-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-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-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-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>

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