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TRV130 hydrochloride

Cat. No. M4808
TRV130 hydrochloride Structure
Synonym:

Oliceridine; TRV130 HCl

Size Price Availability Quantity
2mg USD 120  USD120 In stock
5mg USD 200  USD200 In stock
10mg USD 350  USD350 In stock
50mg USD 850  USD850 In stock
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Quality Control
Biological Activity

TRV130 hydrochloride (Oliceridine) is a functionally selective μ-opioid receptor agonist developed by Trevena Inc.TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine.

Product Citations
Customer Product Validations & Biological Datas
Source Anesthesia & Analgesia (2018 Jul). Figure 5. TRV-130 (Abmole Bioscience Inc, Houston, TX)
Method CPP assay
Cell Lines mice
Concentrations 1.25 or 10 mg/kg
Incubation Time 7 d
Results Figure 5 shows that TLR4 mRNA expression was increased in the lumbar spinal cord tissue of fracture mice that received morphine at 3 weeks after injury(P < .05), while no such changes were observed in the fracture mice by the administration of oliceridine (P> .05).
Source Anesthesia & Analgesia (2018 Jul). Figure 4. TRV-130 (Abmole Bioscience Inc, Houston, TX)
Method CPP assay
Cell Lines mice
Concentrations 5 μL/injection
Incubation Time 7 d
Results The small amount of ethanol in the oliceridine vehicle (5 μL/injection) did not appear to affect nociceptive sensitivity as demonstrated in Figure 4.
Source Anesthesia & Analgesia (2018 Jul). Figure 3. TRV-130 (Abmole Bioscience Inc, Houston, TX)
Method CPP assay
Cell Lines mice
Concentrations 1.25 or 10 mg/kg
Incubation Time 3 d
Results However, a dose of oliceridine providing similar levels of analgesia, 1.25 mg/kg, did not cause statistically significant CPP (P > .05).
Source Anesthesia & Analgesia (2018 Jul). Figure 2. TRV-130 (Abmole Bioscience Inc, Houston, TX)
Method CPP assay
Cell Lines mice
Concentrations 1.25 or 10 mg/kg
Incubation Time 3 d
Results Figure 2 shows that both chronic oliceridine and morphine treatment reduced the mechanical paw withdraw thresholds in comparison with the baseline thresholds (P < .001).
Source Anesthesia & Analgesia (2018 Jul). Figure 1. TRV-130 (Abmole Bioscience Inc, Houston, TX)
Method chronic administration
Cell Lines mice
Concentrations 5 mg/kg twice per day on days 1-3 and on day 4, 10 mg/kg
Incubation Time 4 days
Results Figure 1A, B and the Table show that oliceridine dose–response curves were not significantly changed before and after chronic dosing (P > .05).
Source J Psychopharmacol (2017). Figure 1. TRV130
Method injection
Cell Lines mice
Concentrations 100 nM
Incubation Time 24h
Results In the repeated-vehicle treatment group, vehicle administration on Day 4 did not produce antinociception, and mice displayed high fecal output, whereas 10 mg/kg (+)-TRV130 produced maximal antinociception in all mice and nearly maximal suppression of fecal output. In the 3-day (+)-TRV130 treatment group
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 423.01
Formula C22H31ClN2O2S
CAS Number 1401031-39-7
Purity 99.02%
Solubility DMSO ≥ 35 mg/mL
Storage at -20°C
References

[1] Soergel DG, et al. Pain. Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers.

[2] Violin JD, et al. Trends Pharmacol Sci. Biased ligands at G-protein-coupled receptors: promise and progress.

[3] Soergel DG, et al. J Clin Pharmacol. First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers. Soergel DG1, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW.

[4] Chen XT, et al. J Med Chem. Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.

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Keywords: TRV130 hydrochloride, Oliceridine; TRV130 HCl supplier, Opioid Receptor, inhibitors

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