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Art. -Nr.: HY-184490

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BPR1M492

BPR1M492 is a brain-penetrant μ-opioid receptor (MOR) agonist an in vitro EC₅₀ of 0.93 nM in the cAMP inhibition assay and 0.004 nM in the FLIPR Ca²⁺ assay without a clear signaling bias between cAMP and β-arrestin-2 pathway. BPR1M492 is a cAMP-biased nociceptin-orphanin FQ opioid peptide agonist. BPR1M492 is a weak cAMP-biased δ/κ-opioid receptor agonist. BPR1M492 demonstrates potent in vivo antinociception and can be used for pain research.

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CAS. Nr.: 3118558-91-8
Formel: C₂₁H₂₄N₂O
Molecular Weight:320.43

Speicherung:

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

BPR1M492 Chemical Structure

CAS. Nr.: 3118558-91-8

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

μ Opioid Receptor/MOR

0.93 nM (EC₅₀, the cAMP inhibition assay)

μ Opioid Receptor/MOR

0.004 nM (EC₅₀, the FLIPR Ca²⁺ assay)

NOP Receptor/ORL1

52.89 nM (EC₅₀, the cAMP inhibition assay)

κ Opioid Receptor/KOR

2410 nM (EC₅₀, the FLIPR Ca²⁺ assay)

δ Opioid Receptor/DOR

730 nM (EC₅₀, the cAMP assay)

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

BPR1M492 (compound 56) (336 s) activates MOR of CHO-K1 cells expressing human MOR and Gα15 (CHO-K1/hMOR/Gα15) with 91.7% maximum efficacy^[1].
BPR1M492 fully agonizes MOR with an EC₅₀ of 0.93 nM by the cAMP assay and NOP with an EC₅₀ of 52.89 nM by the cAMP assay^[1].
BPR1M492 weakly agonizes DOR with an EC₅₀ of 730 nM by the cAMP assay and KOR with an EC₅₀ of 2410 nM by the FLIPR Ca2+ assay^[1].
BPR1M492 (CHO-K1 cell) effectively recruits β-arrestin-2 on MOR with an EC₅₀ of 161 nM^[1].
BPR1M492 (CHO-K1 cell) exhibits nearly no effect on β-arrestin-2 recruitment for NOP and KOR, and a partial effect for DOR with an EC₅₀ of 2883 nM^[1].
BPR1M492 fails to block the NMDAR ion channel at 3 μM and inhibits CYP1A, 2B6, 2C8, 2C9, and 3A with IC₅₀s > 100 μM^[1].
BPR1M492 inhibits CYP2C19 with an IC₅₀ of 26 μM and 2D6 with an IC₅₀ of 2.1 μM^[1].
BPR1M492 inhibits hERG with an IC₅₀ of 1.92 μM^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2 (Plasma)	T_1/2 (Brain)	C_max (Brain)	T_max (Plasma)	T_max (Brain)	AUC_0-∞ (Plasma)	AUC_0-∞ (Brain)
Mice^[1]	1 mg/kg	s.c.	0.2 h	0.3 h	1457 ng/g	0.1 h	0.3 h	181 ng·h/mL	856 h·ng/g

In Vivo

BPR1M492 (compound 56) (s.c.; 30-120 min) exhibits the most potent antinociceptive activity in a thermally stimulated mouse tail-flick test with hMOR+ and mMOR-/- mice, which is mediated by MOR activation with an ED₅₀ of 0.027 mg/kg^[1].
BPR1M492 (0.168 mg/kg; s.c.; 12 min) takes effect within approximately 5 minutes after subcutaneous (s.c.) administration in hMOR+ and mMOR-/- mice which indicates that BPR1M492 shows potential as an analgesic for postoperation^[1].
BPR1M492 (0.054 mg/kg-0.162 mg/kg; s.c.; 30-120 min) produces potent antinociception and shows smaller reductions in oxygen saturation and respiratory rate in the incisional pain model in hMOR+ and mMOR-/- mice than TRV130 under the present dosing conditions^[1].
BPR1M492 retains effective antinociception in the incisional pain model in hMOR+ and mMOR-/- mice and shows the clearest improvement in withdrawal-related behaviors in hMOR+ and mMOR-/- mice relative to TRV130^[1].

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

Animal Model:

Mice with pharmacological treatments targeting acute thermal pain^[1].
Dosage:

0.054 mg/kg, 0.108 mg/kg, 0.162 mg/kg
Administration:

s.c.; 120 min
Result:

Increased pain thresholds in a dose-dependent manner in response to thermal.

Animal Model:

The hMOR+ and mMOR-/- mice in the incisional pain model^[1].
Dosage:

0.054 mg/kg, 0.108 mg/kg, 0.162 mg/kg
Administration:

s.c.; 120 min
Result:

Increased pain thresholds in a dose-dependent manner in response to mechanical stimuli.

Animal Model:

Mice were anesthetized with a cocktail of ketamine (100 mg/kg) and xylazine (10 mg/kg) administered intraperitoneally^[1].
Dosage:

0.054 mg/kg, 0.108 mg/kg
Administration:

s.c.; 30 min
Result:

Showed smaller reductions in oxygen saturation and respiratory rate than TRV130 under the present dosing conditions and compensatoryly increased heart rate.

Animal Model:

Male hMOR+; mMOR -/- mice^[1].
Dosage:

0.270 mg/kg
Administration:

s.c.; 30 min
Result:

Demonstrated that adverse effects were abolished in MOR knockout (mMOR-/-) mice, suggesting that the side effects are indeed mediated through the MOR.

Animal Model:

Male C57BL/6J mice^[1].
Dosage:

0.270 mg/kg, 0.054 mg/kg, 0.108 mg/kg, 0.216 mg/kg
Administration:

s.c.; 24 h
Result:

Showed lower CPP responses than TRV130 at some of the tested dose levels (1 × and 8 × ED₅₀) and elicited significant place preference only at medium to high doses (2 × and 4 × ED₅₀).

Animal Model:

Male C57BL/6J mice^[1].
Dosage:

0.054 mg/kg, 0.108 mg/kg, 0.162 mg/kg, 0.216 mg/kg, 0.270 mg/kg
Administration:

twice a day; 5 days
Result:

Elicited only mild withdrawal signs.

Chemical Information

CAS. Nr. 3118558-91-8
Molecular Weight 320.43
Formel C₂₁H₂₄N₂O
SMILES

CN1CC2=CC=CC=C2C[C@@H]1CNC(C3CC(C=CC=C4)=C4C3)=O
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]. Chang PW, et al. Structural Modification and Development of N-(1,2,3,4-Tetrahydro-3-isoquinolinylmethyl)benzamide, BPR1M492, as a Potent and Rapid-Onset Opioid Analgesic with Reduced Withdrawal Symptoms. J Med Chem. 2026 Jun 11;69(11):13222-13247. [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.

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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BPR1M492

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

BPR1M492 Related Classifications

HY-184490 Related Classifications