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Cat. No.: HY-122561

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MK-1925

MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC₅₀ of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel.

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

CAS No.: 932705-04-9
Formula: C₁₉H₂₁F₃N₄
Molecular Weight:362.40

Storage:

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

MK-1925 Chemical Structure

CAS No.: 932705-04-9

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>10 μM Compound: 39, MK-1925	Displacement of [3H]diprenorphin from human cloned mu opioid receptor expressed in CHO cells Displacement of [3H]diprenorphin from human cloned mu opioid receptor expressed in CHO cells	[PMID: 19564110]
CHO	IC₅₀	9800 nM Compound: 39, MK-1925	Displacement of [3H]U69593 from human cloned kappa opioid receptor expressed in CHO cells Displacement of [3H]U69593 from human cloned kappa opioid receptor expressed in CHO cells	[PMID: 19564110]
HEK293	IC₅₀	9500 nM Compound: 39, MK-1925	Displacement of [35S]MK499 from human ERG expressed in HEK293 cells overexpressing Ikr channel protein Displacement of [35S]MK499 from human ERG expressed in HEK293 cells overexpressing Ikr channel protein	[PMID: 19564110]

In Vitro

MK-1925 (compound 39) is highly selective for ORL1 receptors over human μ, κ, and δ opioid receptors, with ORL1 binding IC₅₀ of 8.2 nM and minimal binding to other opioid receptors (IC₅₀ values ≥9800 nM or >10,000 nM)^[1].
MK-1925 has minimal binding affinity for hERG potassium channels, with an IC₅₀ of 9500 nM^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	V_dss	AUC_0-inf	C_max	T_1/2	Bioavailability
Rat^[1]	1 mg/kg	i.v.	83 mL/min/kg	5.2 L/kg	/	/	/	/
Rat^[1]	3 mg/kg	p.o.	/	/	0.3 μM·h	0.40 μM	0.7 h	21 %
Dog^[1]	1 mg/kg	i.v.	37 mL/min/kg	3.5 L/kg	/	/	/	/
Dog^[1]	3 mg/kg	p.o.	/	/	1.3 μM·h	2.6 μM	2.8 h	/

Chemical Information

CAS No. 932705-04-9
Molecular Weight 362.40
Formula C₁₉H₂₁F₃N₄
SMILES

C(CC#N)N1C(=C(C)C(CN[C@@H]2C[C@H](F)CC2)=N1)C3=CC(F)=CC(F)=C3
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

Handling Instructions (2659 KB)

References

[1]. Kobayashi K, et al. Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. Bioorg Med Chem Lett. 2009;19(16):4729-4732. [Content Brief]

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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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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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MK-1925

All Opioid Receptor Isoforms