Free shipping on all orders over $ 500

TRV130 hydrochloride

Cat. No. M4808
TRV130 hydrochloride Structure
Synonym:

TRV130 HCl

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 350 In stock
50mg USD 900 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

TRV 130 hydrochloride 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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 423.01
Formula C22H31ClN2O2S
CAS Number 1401031-39-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

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.
Soergel DG, et al. Pain. 2014 Sep;155(9):1829-35. PMID: 24954166.

Biased ligands at G-protein-coupled receptors: promise and progress.
Violin JD, et al. Trends Pharmacol Sci. 2014 Jul;35(7):308-16. PMID: 24878326.

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.
Soergel DG, et al. J Clin Pharmacol. 2014 Mar;54(3):351-7. PMID: 24122908.

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.
Chen XT, et al. J Med Chem. 2013 Oct 24;56(20):8019-31. PMID: 24063433.

Related Opioid Receptor Products
Trimebutine maleate

Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects.

Trimebutine

Trimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.

Docusate Sodium

Docusate Sodium is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.

Alvimopan dihydrate

Alvimopan dihydrate(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

PZM21

PZM21 is a potent and selective μ-opioid-receptor (μOR) agonist with an EC50 of 1.8 nM.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.