country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-122561

Copy Link Print Information

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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 932705-04-9
Formule: C₁₉H₂₁F₃N₄
Masse moléculaire:362.40

Stockage:

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

MK-1925 Chemical Structure

CAS No.: 932705-04-9

Size

Prix

Stock

Quantité

Amount: USD 0.00

* Veuillez sélectionner la quantité avant d'ajouter des articles.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Opioid Receptor :

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
Masse moléculaire 362.40
Formule C₁₉H₂₁F₃N₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Obtenir un devis En stock

Other size

Obtenir un devis

Amount: USD 0.00

Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
Références

Nom du produit:
Cat. No.:
Quantité:
MCE Japan Authorized Agent:

Nom du produit:
CAS No.:
Species:
Pureté:
Quantité:

MK-1925

Voir tous les produits spécifiques à Isoform Opioid Receptor