| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Angiotensin II Type 1
Angiotensin II receptor type 1 (AT1R). |
|---|---|
| ln Vitro |
TRV055 is a "gain-of-function" biased agonist that shows increased allosteric coupling to Gq compared to AngII. It is highly efficacious at stimulating cellular Gq-mediated signaling while exhibiting similar beta-arrestin coupling to the endogenous ligand.
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| ln Vivo |
TRV055 has been used in vivo to study the distinct physiological and pathophysiological contributions of Gq-dependent signaling versus beta-arrestin-dependent signaling at the AT1 receptor. Its effects are primarily mediated by Gq activation.
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| Enzyme Assay |
A competitive radioligand binding assay is performed. Membranes from cells overexpressing AT1R are incubated with a radiolabeled antagonist (e.g., 125I-[Sar1, Ile8]-AngII) and varying concentrations of TRV055. Specific binding is measured to calculate the Ki value.
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| Cell Assay |
HEK293 cells expressing AT1R are treated with TRV055 (0.1 nM-10 microM) for 1 hour. Gq pathway activation is quantified by measuring the accumulation of inositol-1-phosphate (IP1) using a homogeneous time-resolved fluorescence (HTRF) assay kit. The EC50 for Gq signaling is determined.
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| Animal Protocol |
In vivo, TRV055 can be administered intravenously to rodents to study acute hemodynamic effects. However, it is more commonly used in ex vivo settings with tissue samples to study AT1R signal transduction independent of confounding systemic factors.
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| ADME/Pharmacokinetics |
As a peptide-based biased agonist, TRV055 is expected to have a short half-life in vivo due to rapid proteolytic degradation. It is typically administered via injection as it has poor oral bioavailability. Standard PK studies would require LC-MS/MS quantification.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TRV055 is limited. In cell-based assays at concentrations required for Gq activation (nM to low microM), it does not exhibit cytotoxicity. In vivo studies at pharmacologically relevant doses have not reported acute toxicity.
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| References | |
| Additional Infomation |
TRV055 is a valuable research tool for dissecting the complex signaling pathways of the angiotensin II receptor. Its biased agonism allows for the investigation of which downstream pathways (Gq vs. beta-arrestin) are responsible for specific physiological outcomes.
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| Molecular Formula |
C42H57N9O9
|
|---|---|
| Molecular Weight |
831.956889867783
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| Exact Mass |
831.427
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| CAS # |
25849-90-5
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| Related CAS # |
TRV055 hydrochloride
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| PubChem CID |
50902297
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| Appearance |
White to off-white solid powder
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| LogP |
0.3
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| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
21
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| Heavy Atom Count |
60
|
| Complexity |
1470
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C(N1CCC[C@H]1C(=O)N[C@H](C(=O)O)CC1C=CC=CC=1)(=O)[C@@H](NC(=O)[C@]([H])([C@@H](C)CC)NC(=O)[C@@H](NC(=O)[C@H](C(C)C)NC(=O)CN)CC1C=CC(O)=CC=1)CC1N=CNC=1
|
| InChi Key |
YAJPGWCDYDATRI-DIUSPMSXSA-N
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| InChi Code |
InChI=1S/C42H57N9O9/c1-5-25(4)36(50-37(54)30(18-27-13-15-29(52)16-14-27)46-39(56)35(24(2)3)49-34(53)21-43)40(57)47-31(20-28-22-44-23-45-28)41(58)51-17-9-12-33(51)38(55)48-32(42(59)60)19-26-10-7-6-8-11-26/h6-8,10-11,13-16,22-25,30-33,35-36,52H,5,9,12,17-21,43H2,1-4H3,(H,44,45)(H,46,56)(H,47,57)(H,48,55)(H,49,53)(H,50,54)(H,59,60)/t25-,30-,31-,32-,33-,35-,36-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2020 mL | 6.0099 mL | 12.0198 mL | |
| 5 mM | 0.2404 mL | 1.2020 mL | 2.4040 mL | |
| 10 mM | 0.1202 mL | 0.6010 mL | 1.2020 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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