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TRV-120027

TRV-120027 is an investigational drug designed as a selective, orally bioavailable, small molecule that inhibits the activity of the TRPC5 ion channel.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
TRV-120027(CAS 1234510-46-3)

CAT No: R1867

CAS No:1234510-46-3

Synonyms/Alias:TRV-120027;1234510-46-3;trv027;TRV120027;TRV-027;UNII-J1J4P3PQZD;TRV 027;J1J4P3PQZD;TRV 120027;D-Alanine, N-methylglycyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-;Sar-val-tyr-ile-his-pro-d-ala-oh;(2R)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid;Sar-Arg-Val-Tyr-Ile-His-Pro-Ala;GTPL6902;CHEMBL4297447;TRV 027 [WHO-DD];GLXC-27746;HY-P2141;AKOS040764215;DB12199;NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla;DA-58776;CS-0109050;NS00073768;G17966;Q27281029;

Chemical Name:(2R)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid

Custom Peptide Synthesis
cGMP Peptide
  • Registration of APIs
  • CMC information required for an IND
  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C43H67N13O10
M.W/Mr.
926.1
Sequence
One Letter Code:GRVYIHPA
Three Letter Code:H-Sar-Arg-Val-Tyr-Ile-His-Pro-D-Ala-OH
Application
TRV120027 has been used in trials studying the treatment of Heart Failure and Kidney Disease.
Long-term Storage Conditions
10 mM in DMSO
Shipping Condition
+20°C (International: -20°C)
InChI
InChI=1S/C43H67N13O10/c1-7-24(4)35(40(63)53-31(19-27-20-47-22-49-27)41(64)56-17-9-11-32(56)38(61)50-25(5)42(65)66)55-37(60)30(18-26-12-14-28(57)15-13-26)52-39(62)34(23(2)3)54-36(59)29(51-33(58)21-46-6)10-8-16-48-43(44)45/h12-15,20,22-25,29-32,34-35,46,57H,7-11,16-19,21H2,1-6H3,(H,47,49)(H,50,61)(H,51,58)(H,52,62)(H,53,63)(H,54,59)(H,55,60)(H,65,66)(H4,44,45,48)/t24-,25+,29-,30-,31-,32-,34-,35-/m0/s1
InChI Key
XIEWFECSPPTVQN-KMIMAYJXSA-N
Canonical SMILES
CCC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)N2CCCC2C(=O)NC(C)C(=O)O)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(C(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)CNC
Isomeric SMILES
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(=O)O)NC(=O)[C@H](CC3=CC=C(C=C3)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC
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.
[2]. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9; 8:14335.

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