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Cat. No.: HY-179282

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Mu opioid receptor antagonist 9

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a K_i of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).

For research use only. We do not sell to patients.

CAS No.: 3058600-77-1
Formula: C₂₁H₂₇ClN₂O₂
Molecular Weight:374.90

Storage:

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

Data Sheet (276 KB)

Mu opioid receptor antagonist 9 Chemical Structure

CAS No.: 3058600-77-1

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

μ Opioid Receptor/MOR

77.3 nM (Ki)

κ Opioid Receptor/KOR

681 nM (Ki)

δ Opioid Receptor/DOR

4182 nM (Ki)

All Opioid Receptor Isoforms :

In Vitro

Mu opioid receptor antagonist 9 (compound 53) (15 min) inhibits calcium flux induced by DAMGO (HY-P0210) and psychoactive substances in mMOR-CHO cells with IC₅₀ values of 33.6 and 4.51 μM, respectively^[1].

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

Parmacokinetics

Species	Dose	Route	Plasma Concentration	Brain Concentration	Brain-to-Plasma Ratio
Mice^[1]	10 mg/kg	s.c.	0.97 μg/mL	720 ng/g	0.74
Mice^[1]	10 mg/kg	s.c.	0.80 μg/mL	640 ng/g	0.80
Mice^[1]	10 mg/kg	s.c.	0.66 μg/mL	820 ng/g	1.24
Mice^[1]	10 mg/kg	s.c.	0.58 μg/mL	480 ng/g	0.82

In Vivo

Mu opioid receptor antagonist 9 (1-10 mg/kg; s.c.; single dose) blocks the antinociceptive effects of Morphine and fentanyl in the warm water tail immersion pain model in mice^[1].
Mu opioid receptor antagonist 9 (1-32 mg/kg; s.c.; single dose at 20min post-fentanyl) demonstrates a potent reversal effect on fentanyl-induced respiratory depression in the whole-body plethysmography study in mice^[1].

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

Animal Model:

Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances^[1]
Dosage:

1, 2, 4, 5, 10 mg/kg
Administration:

s.c.; single dose
Result:

Blocked the antinociception of morphine at a dose of 10 mg/kg. showed AD₅₀s of 2.02 mg/kg (95% CL) against 10 mg/kg morphine, and 4.02 mg/kg (95% CL) against 0.1 mg/kg fentanyl.

Animal Model:

Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances^[1]
Dosage:

1, 3.2, 10, 32 mg/kg
Administration:

s.c.; single dose at 20min post-fentanyl
Result:

Demonstrated a potent reversal effect on fentanyl-induced respiratory depression at both 10 and 32 mg/kg doses. Increased both respiratory frequency and tidal volume. Showed beneficial effect within a short time frame, appearing 10 min postadministration for the 32 mg/kg dose and 15 min postadministration for the 10 mg/kg dose.

Chemical Information

CAS No. 3058600-77-1
Molecular Weight 374.90
Formula C₂₁H₂₇ClN₂O₂
SMILES

C=CCN(CCC1)CCCC1N(C(C2=COC=C2)=O)C3=CC=CC=C3.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Silte AA, et al. Design, Syntheses, and Pharmacological Evaluations of Core Ring Expanded Fentanyl Analogues as Potential Counteracting Agents Against Fentanyl Induced Respiratory Depression. J Med Chem. 2025;68(21):22170-22195. [Content Brief]

Calculators

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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.

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MOQ

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100 mg

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