NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla
- Product Name
- NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla
- CAS No.
- 1234510-46-3
- Chemical Name
- NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla
- Synonyms
- TRV-120027;NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla;Sar-Arg-Vla-Tyr-Ile-His-Pro-D-Ala-OH;D-Alanine, N-methylglycyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-
- CBNumber
- CB45849303
- Molecular Formula
- C43H67N13O10
- Formula Weight
- 926.07
- MOL File
- 1234510-46-3.mol
NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla Property
- Density
- 1.41±0.1 g/cm3(Predicted)
- pka
- 3.70±0.10(Predicted)
- form
- Solid
- color
- White to off-white
NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla Chemical Properties,Usage,Production
Uses
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling[1]. 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[2].
in vivo
TRV120027 (intravenous?injection; 0.3 or 1.5 μg/kg per minute; infusion rate, 0.5 mL/min) when added to furosemide decreases cardiac preload and afterload, systemic and renal vascular resistances, and left ventricular external work while increasing cardiac output and renal blood flow. GFR and renal excretory function are maintained in canines with experimental HF[1].
| Animal Model: | Male mongrel dogs (weight, 20.5–30 kg)[1] |
| Dosage: | 0.3 or 1.5 μg/kg per minute; infusion rate, 0.5 mL/min |
| Administration: | Intravenous?injection |
| Result: | Resulted in dose-dependent vasodilation, increased cardiac contractility, and decreased myocardial oxygen consumption in dog. |
IC 50
AT1 Receptor
References
[1] Boerrigter G, et al. TRV120027, a novel β-arrestin biased ligand at the angiotensin II type I receptor, unloads the heart and maintains renal function when added to furosemide in experimental heart failure.Circ Heart Fail. 2012 Sep 1;5(5):627-34. Epub 2012 Aug 13. DOI:10.1161/CIRCHEARTFAILURE.112.969220
[2] Liu CH, et al. Arrestin-biased?AT1R?agonism?induces?acute?catecholamine?secretion?through?TRPC3?coupling.Nat Commun.?2017 Feb 9;8:14335. DOI:10.1038/ncomms14335
NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla Preparation Products And Raw materials
Raw materials
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