TRV-120027 (also known as TRV027) is an angiotensin II receptor type 1 (AT1R) antagonist and engages ß-arrestins while blocking G-protein signaling. TRV-120027 TFA (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. TRV-120027 TFA (i.v.; 0.3 or 1.5 µg/kg per minute, diluted in saline; infusion rate, 0.5 mL/min), when added to furosemide, decreases cardiac preload and afterload, systemic and renal vascular resistance, and left ventricular external work while increasing cardiac output and renal blood flow.
Clin Sci (Lond). 2023 Dec 5;CS20230313.
β-arrestin pathway activation by selective ATR1 agonism promotes calcium influx in podocytes, leading to glomerular damage
TRV-120027 TFA purchased from AbMole
| Molecular Weight | 1040.1 |
| Formula | C45H68F3N13O12 |
| CAS Number | 1234510-46-3 (free base) |
| Solubility (25°C) | DMSO ≥ 60 mg/mL Water ≥ 1 mg/mL |
| Storage | -20°C, dry, sealed, protect from light |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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