TRV027, Type-1 angiotensin II receptor antagonist, CAS No.1234510-46-3, Type-1 angiotensin II receptor antagonist

Features and benefits
In stock
Item Number
rp175328
Grouped product items
SKU Size Availability Price Qty
rp175328-500μg
500μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,334.90
rp175328-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,334.90
View related series
AT1 receptor Antagonist (0)

Basic Description

Product Name TRV027, Type-1 angiotensin II receptor antagonist, CAS No.1234510-46-3
Synonyms CS-0109050 | TRV 027 [WHO-DD] | Sar-val-tyr-ile-his-pro-d-ala-oh | TRV120027 | TRV-120027 | D-Alanine, N-methylglycyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl- | TRV 027 | trv027 | TRV-027 | AKOS040764215 | TRV 120027 | UNII-J1J4P3PQZD
Grade Moligand™
Specifications & Purity Moligand™
Action Type ANTAGONIST
Mechanism of action Type-1 angiotensin II receptor antagonist

AI Insight

Product Properties

ALogP -2.3

Associated Targets(Human)

AGTR1 Tclin Type-1 angiotensin II receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Agtr1 Type-1A angiotensin II receptor (520 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Product Specifications

CAS 1234510-46-3

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Specifications

Genetic information

Alternate Names CS-0109050 | TRV 027 [WHO-DD] | Sar-val-tyr-ile-his-pro-d-ala-oh | TRV120027 | TRV-120027 | D-Alanine, N-methylglycyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl- | TRV 027 | trv027 | TRV-027 | AKOS040764215 | TRV 120027 | UNII-J1J4P3PQZD
Reference
  • 1. Kinetics and inhibition of recombinant human cystathionine gamma-lyase. Toward the rational control of transsulfuration., The Journal of biological chemistry, Steegborn, C C and 7 more authors.
  • 2. Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences., Proceedings of the National Academy of Sciences of the United States of America, Strausberg, Robert L RL and 83 more authors.
  • 3. Genomic basis of cystathioninuria (MIM 219500) revealed by multiple mutations in cystathionine gamma-lyase (CTH)., Human genetics, Wang, Jian J and Hegele, Robert A RA.
  • 4. Cloning and nucleotide sequence of human liver cDNA encoding for cystathionine gamma-lyase., Biochemical and biophysical research communications, Lu, Y Y, O'Dowd, B F BF, Orrego, H H and Israel, Y Y.
  • 5. Single nucleotide polymorphism in CTH associated with variation in plasma homocysteine concentration., Clinical genetics, Wang, J J, Huff, A M AM, Spence, J D JD and Hegele, R A RA.
  • 6. Cystathionine gamma-lyase overexpression inhibits cell proliferation via a H2S-dependent modulation of ERK1/2 phosphorylation and p21Cip/WAK-1., The Journal of biological chemistry, Yang, Guangdong G, Cao, Kun K, Wu, Lingyun L and Wang, Rui R.
  • 7. The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)., Genome research, Gerhard, Daniela S DS and 115 more authors.
  • 8. Towards a proteome-scale map of the human protein-protein interaction network., Nature, Rual, Jean-François JF and 37 more authors.
  • 9. The DNA sequence and biological annotation of human chromosome 1., Nature, Gregory, S G SG and 178 more authors.
  • 10. Polymorphisms in one-carbon metabolism and trans-sulfuration pathway genes and susceptibility to bladder cancer., International journal of cancer, Moore, Lee E LE and 14 more authors. more

References

1. Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M, Lark MW.  (2010)  Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance..  J Pharmacol Exp Ther,  335  (3): (572-9).  [PMID:20801892] [10.1021/op500134e]
2. Boerrigter G, Lark MW, Whalen EJ, Soergel DG, Violin JD, Burnett Jr JC.  (2011)  Cardiorenal actions of TRV120027, a novel ß-arrestin-biased ligand at the angiotensin II type I receptor, in healthy and heart failure canines: a novel therapeutic strategy for acute heart failure..  Circ Heart Fail,  (6): (770-8).  [PMID:21835984] [10.1021/op500134e]
3. Boerrigter G, Soergel DG, Violin JD, Lark MW, Burnett Jr JC.  (2012)  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,  (5): (627-34).  [PMID:22891045] [10.1021/op500134e]
4. Pang PS, Butler J, Collins SP, Cotter G, Davison BA, Ezekowitz JA, Filippatos G, Levy PD, Metra M, Ponikowski P et al..  (2017)  Biased ligand of the angiotensin II type 1 receptor in patients with acute heart failure: a randomized, double-blind, placebo-controlled, phase IIB, dose ranging trial (BLAST-AHF)..  Eur Heart J,  38  (30): (2364-2373).  [PMID:28459958] [10.1021/op500134e]
5. Soergel DG, Subach RA, Cowan CL, Violin JD, Lark MW.  (2013)  First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers..  J Clin Pharmacol,  53  (9): (892-9).  [PMID:23813302] [10.1021/op500134e]

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