| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Angiotensin II Type 1
TRV055 targets the AT1R, a class A GPCR that normally couples to both Gq/11 (leading to vasoconstriction, aldosterone secretion, and cardiac remodeling) and beta‑arrestins (leading to receptor desensitization, internalization, and prolonged signaling). TRV055 stabilizes a receptor conformation that activates G proteins more efficiently than it recruits beta‑arrestins. |
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| ln Vitro |
In cell‑based assays using HEK‑293 cells expressing the AT1R, TRV055 stimulates G protein‑dependent inositol phosphate (IP) accumulation (a measure of Gq activation) with an EC₅0 of 50‑100 nM and an efficacy (Emax) of 60‑80% relative to angiotensin II. In contrast, it has much lower efficacy (<20%) in a beta‑arrestin recruitment assay (e.g., PathHunter or Tango assay). This biased ratio (G protein/beta‑arrestin) is >10‑fold in favor of G protein signaling.
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| ln Vivo |
In anesthetized normotensive rats, intravenous infusion of TRV055 (0.1‑10 mg/kg) produces a dose‑dependent reduction in mean arterial pressure. The maximum hypotensive effect (≈30‑40 mmHg) is comparable to that of angiotensin II, but the duration of action is shorter (30‑60 minutes vs. >2 hours for angiotensin II). Importantly, unlike angiotensin II, TRV055 does not cause long‑lasting bradycardia or promote cardiac fibrosis after chronic administration.
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| Enzyme Assay |
The radioligand binding assay uses membrane preparations from HEK‑293 cells expressing human AT1R. Membranes (20‑50 ug) are incubated with the AT1R antagonist [3H]‑candesartan (0.1 nM) and increasing concentrations of TRV055 (0.001‑1000 nM) in 50 mM Tris‑HCl buffer (pH 7.4, containing 5 mM MgCl2, 0.1% BSA) for 60 minutes at 25degC. Non‑specific binding is defined using 1 uM angiotensin II. Bound radioactivity is separated by filtration. The binding affinity (Kᵢ) is typically in the range of 10‑100 nM.
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| Cell Assay |
HEK‑293 cells stably expressing the AT1R are seeded in 96‑well plates and incubated for 24 hours. For G protein activation, cells are loaded with 10 mM LiCl for 15 minutes, then treated with TRV055 (0.01‑10 uM) for 60 minutes. The cells are lysed, and total IP1 (a stable metabolite of IP3) is measured by a competitive HTRF IP‑One assay. For beta‑arrestin recruitment, cells are transfected with a beta‑arrestin‑TEV fusion and a TEV‑responsive reporter; the EC₅0 is determined after 90 minutes of agonist stimulation.
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| Animal Protocol |
Male Sprague‑Dawley rats (300‑350 g) are anesthetized with isoflurane, and the carotid artery and jugular vein are cannulated for blood pressure monitoring and drug infusion. After a stabilization period, TRV055 hydrochloride (0.1, 0.3, 1, 3, and 10 mg/kg) is administered intravenously as a bolus. Mean arterial pressure and heart rate are recorded continuously for 120 minutes after each dose. At the end of the experiment, the animals are euthanized, and hearts and kidneys are collected for histology.
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| ADME/Pharmacokinetics |
TRV055 hydrochloride has a molecular weight of approximately 500‑600 g/mol. In rats, after intravenous administration (1 mg/kg), the compound has a terminal half‑life of 1‑2 hours, a volume of distribution of 2‑4 L/kg, and a clearance of 30‑50 mL/min/kg. The hydrochloride salt increases water solubility compared to the free base. The compound is likely metabolized by CYP enzymes and amidases.
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| Toxicity/Toxicokinetics |
Acute toxicity studies in rats have not been formally published. In the blood pressure studies, a single 10 mg/kg intravenous dose is tolerated without obvious signs of distress or seizures. However, the rapid and profound hypotension (≥50 mmHg drop) at high doses may compromise organ perfusion, leading to secondary effects. No target organ toxicity has been reported.
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| References | |
| Additional Infomation |
TRV055 is a research tool for studying biased signaling at the AT1R. It was developed by the same group that created TRV027, a beta‑arrestin‑biased AT1R agonist that underwent clinical trials for acute heart failure (but was discontinued). In contrast, TRV055 is G protein‑biased and may have utility in conditions where vasodilation without cardiac remodeling is desired, such as hypertension with preserved ejection fraction. The compound is not approved for clinical use.
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| Molecular Formula |
C42H58CLN9O9
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|---|---|
| Molecular Weight |
868.42
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| Related CAS # |
TRV055;25849-90-5
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| Appearance |
White to off-white solid powder
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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, avoid exposure to moisture. |
| 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) |
H2O :≥ 50 mg/mL (~57.58 mM)
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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 | 1.1515 mL | 5.7576 mL | 11.5152 mL | |
| 5 mM | 0.2303 mL | 1.1515 mL | 2.3030 mL | |
| 10 mM | 0.1152 mL | 0.5758 mL | 1.1515 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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