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Art. -Nr.: HY-120925

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TRV0109101

Name: TRV0109101
Brand: MedChemExpress
SKU: HY-120925
Price: 390.00 USD
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TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (K_D = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research.

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CAS. Nr.: 1401027-29-9
Formel: C₂₁H₂₈N₂OS
Molecular Weight:356.53

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

TRV0109101 Chemical Structure

CAS. Nr.: 1401027-29-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

human μ-opioid receptor

70 nM (Kd)

Arrestin-2/β-Arrestin 1

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.75 μM Compound: (R)-19	Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	[PMID: 24063433]
HEK293	IC₅₀	100 μM Compound: (R)-19	Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique	[PMID: 24063433]
HEK293	EC₅₀	0.9 μM Compound: (R)-19	Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay	[PMID: 24063433]
HEK293	IC₅₀	>100 μM Compound: (R)-19	Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique	[PMID: 24063433]
HEK293	IC₅₀	2.3 μM Compound: (R)-19	Inhibition of human ERG channel expressed in HEK293 cells by whole-cell patch clamp technique Inhibition of human ERG channel expressed in HEK293 cells by whole-cell patch clamp technique	[PMID: 24063433]
HEK293	IC₅₀	20 μM Compound: (R)-19	Inhibition of human Nav 1.5 tonic ion channel expressed in HEK293 cells by whole-cell patch clamp technique Inhibition of human Nav 1.5 tonic ion channel expressed in HEK293 cells by whole-cell patch clamp technique	[PMID: 24063433]
HEK293	IC₅₀	9 μM Compound: (R)-19	Inhibition of human Nav 1.5 phasic ion channel expressed in HEK293 cells by whole-cell patch clamp technique Inhibition of human Nav 1.5 phasic ion channel expressed in HEK293 cells by whole-cell patch clamp technique	[PMID: 24063433]

In Vitro

TRV0109101 acts as a potent, G protein-biased, MOPR-selective agonist in HEK-293 cells, with an EC₅₀ of 10 nM for cAMP inhibition^[1].
TRV0109101 (41 nM-10 μM; 5 min) interacts with the orthosteric ligand binding site of human MOPR in HEK-293 cells, with an apparent K_D of 70 nM in competition with DAMGO for β-arrestin2 recruitment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TRV0109101 (20 mg/kg/day; s.c.; continuous infusion; 7 days) does not promote opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance^[1].
TRV0109101 (20-40 mg/kg; s.c.; twice daily (days 1-3), single double dose (day 4); 5 days) does not induce opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance^[1].
TRV0109101 (20 mg/kg; s.c.; twice daily; 7 days) rapidly reverses mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops^[1].
TRV0109101 (1-3 mg/kg; s.c.; twice daily) rapidly and fully reverses induced mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops^[1].
TRV0109101 (0.1-10 mg/kg; s.c.; single dose) produces dose-dependent antinociception in the mouse 56°C hot plate assay, with an ED₅₀ of 1.1 mg/kg^[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of fecal boli accumulation in male C57BL/6 mice, with an ED₅₀ of 6.3 mg/kg^[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of colonic motility in male C57BL/6 mice, with an ED₅₀ of 9.4 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (8 to 10-week-old male, opioid-induced mechanical allodynia model via chronic minipump infusion of μ-opioid agonists over 7 days)^[1]
Dosage:

20 mg/kg/day
Administration:

s.c.; continuous infusion; 7 days
Result:

Did not induce significant mechanical allodynia over the 7-day period.
Developed antinociceptive tolerance to thermal stimuli comparable to that seen with conventional opioids.

Animal Model:

C57BL/6 (8 to 10-week-old male, opioid-induced mechanical allodynia model via twice-daily subcutaneous dosing on days 1-3, with a double dose on day 4)^[1]
Dosage:

20 mg/kg (days 1-3); 40 mg/kg (day 4)
Administration:

s.c.; twice daily (days 1-3); single double dose (day 4); 5 days
Result:

Did not develop opioid-induced mechanical allodynia over the 5-day treatment period.
Developed antinociceptive tolerance comparable to that seen with conventional opioids.

Animal Model:

C57BL/6 (8 to 10-week-old male, morphine-induced mechanical allodynia reversal model)^[1]
Dosage:

20 mg/kg
Administration:

s.c.; twice daily; 7 days
Result:

Attenuated morphine-induced mechanical allodynia within 24 hours of treatment initiation, with levels indistinguishable from vehicle-treated animals.
Developed antinociceptive tolerance.

Animal Model:

C57BL/6 (8 to 10-week-old male, fentanyl-induced mechanical allodynia reversal model)^[1]
Dosage:

1 mg/kg; 3 mg/kg
Administration:

s.c.; twice daily
Result:

Fully reversed fentanyl-induced mechanical allodynia within 1 day of treatment initiation at both doses, with levels indistinguishable from vehicle-treated animals by days 7-8.
Developed antinociceptive tolerance.

Animal Model:

C57BL/6 (8 to 10-week-old male, acute pain model via 56°C hot plate assay)^[1]
Dosage:

0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

s.c.; single dose
Result:

Produced dose-dependent antinociception, with an ED₅₀ of 1.1 mg/kg.
Resulted in significant increases in percent maximum possible effect (%MPE) compared to vehicle at doses of 1 mg/kg, 3 mg/kg, and 10 mg/kg.

Animal Model:

C57BL/6 (8 to 10-week-old male, gastrointestinal function impairment model via fecal boli accumulation assay)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

s.c.; single dose
Result:

Produced dose-dependent reduction in fecal boli weight, with an ED₅₀ of 6.3 mg/kg.
Resulted in significant decreases in fecal boli weight compared to vehicle at doses of 10 mg/kg and 20 mg/kg.

Animal Model:

C57BL/6 (8 to 10-week-old male, gastrointestinal function impairment model via glass bead colonic motility assay)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

s.c.; single dose
Result:

Produced dose-dependent increases in colonic transit time, with an ED₅₀ of 9.4 mg/kg.
Resulted in significant increases in transit time compared to vehicle at doses of 1 mg/kg, 3 mg/kg, 10 mg/kg, and 20 mg/kg.

Chemical Information

CAS. Nr. 1401027-29-9
Molecular Weight 356.53
Formel C₂₁H₂₈N₂OS
SMILES

C(CNCC1=CC=CS1)[C@@]2(CC3(OCC2)CCCC3)C4=CC=CC=N4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Koblish M, et al. TRV0109101, a G Protein-Biased Agonist of the µ-Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration. J Pharmacol Exp Ther. 2017;362(2):254-262. [Content Brief]

[2]. Chen XT, et al. 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. J Med Chem. 2013;56(20):8019-8031. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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TRV0109101

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