TRV-120027
Based on 3 publication(s) in Google Scholar
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-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.
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- Purity: 98.21%
- CAS No.: 1234510-46-3
- 화학식: C43H67N13O10
- 분자량:926.07
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보관:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TRV-120027
MoreAll Angiotensin Receptor Isoforms
MoreAll Arrestin Isoforms
More
Biological Activity
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AT1 Receptor |
Arrestin-2/β-Arrestin 1 |
TRV120027 (100 nM) significantly increases the AT1R and TRPC3 association with the immunoprecipitated β-arrestin-1 in HEK293 cells co-transfected with Flag-AT1R-cherry, HA-β-arrestin-1 and TRPC3-GFP[2]. TRV120027 (100 nM) induces an [Ca2+]i increase in HEK293 cells co-transfected with AT1R, β-arrestin-1, and TRPC3, which are significantly blocked by Pyr3 pre-incubation in HEK293 cells co-transfected with Flag-AT1R-Cherry, HA-β-arrestin-1, and TRPC3-GFP[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mongrel dogs (weight, 20.5–30 kg)[1]
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Dosage:0.3 or 1.5 µg/kg per minute; infusion rate, 0.5 mL/min
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Administration:Intravenous injection
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Result:Resulted in dose-dependent vasodilation, increased cardiac contractility, and decreased myocardial oxygen consumption in dog.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1234510-46-3
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Appearance Solid
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분자량 926.07
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화학식 C43H67N13O10
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Color White to off-white
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Synonyms
TRV027
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Sequence Shortening
{Sar}-RVYIHP-{d-Ala}
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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J Am Heart Assoc
Myogenic Vasoconstriction Requires Canonical Gq/11 Signaling of the Angiotensin II Type 1 Receptor. [Abstract]2022 Feb 15;11(4):e022070. PMID: 35132870 -
Eur J Pharmacol
Gαq protein-biased ligand of angiotensin II type 1 receptor mediates myofibroblast differentiation through TGF-β1/ERK axis in human cardiac fibroblasts. [Abstract]2023 Jul 15:951:175780. PMID: 37209939 -
용액&용해도
H2O : 100 mg/mL (107.98 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.0798 mL | 5.3992 mL | 10.7983 mL | 26.9958 mL |
| 5 mM | 0.2160 mL | 1.0798 mL | 2.1597 mL | 5.3992 mL | |
| 10 mM | 0.1080 mL | 0.5399 mL | 1.0798 mL | 2.6996 mL | |
| 15 mM | 0.0720 mL | 0.3599 mL | 0.7199 mL | 1.7997 mL | |
| 20 mM | 0.0540 mL | 0.2700 mL | 0.5399 mL | 1.3498 mL | |
| 25 mM | 0.0432 mL | 0.2160 mL | 0.4319 mL | 1.0798 mL | |
| 30 mM | 0.0360 mL | 0.1800 mL | 0.3599 mL | 0.8999 mL | |
| 40 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6749 mL | |
| 50 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5399 mL | |
| 60 mM | 0.0180 mL | 0.0900 mL | 0.1800 mL | 0.4499 mL | |
| 80 mM | 0.0135 mL | 0.0675 mL | 0.1350 mL | 0.3374 mL | |
| 100 mM | 0.0108 mL | 0.0540 mL | 0.1080 mL | 0.2700 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
TRV-120027 Related Classifications
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