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Art. -Nr.: HY-182384

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VU6015241

VU6015241 is a selective, blood-brain barrier-permeable M4 mAChR Antagonist with a K_i value of 43.3 nM. VU6015241 is used for the research of dystonia and related movement disorders.

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CAS. Nr.: 2264025-00-3
Formel: C₂₆H₃₅N₅O₂
Molecular Weight:449.59

Speicherung:

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

VU6015241 Chemical Structure

CAS. Nr.: 2264025-00-3

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

VU6015241 is a selective, blood-brain barrier-permeable M4 mAChR Antagonist with a K_i value of 43.3 nM. VU6015241 is used for the research of dystonia and related movement disorders^[1].

IC₅₀ & Target^[1]

mAChR4

43.3 nM (Ki)

Alle mAChR Isoform-spezifische Produkte anzeigen :

In Vitro

VU6015241 potently inhibits acetylcholine-stimulated calcium mobilization in hM₄/Gqi5-CHO cells with an IC₅₀ of 71 nM^[1].
VU6015241 inhibits acetylcholine-stimulated calcium mobilization in rM₄-CHO cells with an IC₅₀ of 44 nM^[1].
VU6015241 is highly selective for human and rat M₄ receptors, with IC₅₀ values >10,000 nM at hM₁, hM₂, rM₁, rM₂, rM₃, and rM₅ receptors expressed in CHO cells^[1].
VU6015241 has a predicted low rat hepatic clearance of 6.2 mL/min/kg^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	V_ss	T_1/2 (Elimination)	MRT	AUC_0-last	AUC_0-∞
Rat^[1]	3 mg/kg	i.v.	257 mL/min/kg	147 L/kg	8.6 h	9.33 h	181 ng·h/mL	202 ng·h/mL

In Vivo

VU6015241 (3-30 mg/kg; i.v., i.p.; single dose) administered intravenously at 3 mg/kg to rats shows high plasma clearance of 257 mL/min/kg and a long elimination half-life of 8.6 h, while intraperitoneal administration at 30 mg/kg results in moderate brain exposure with a K_p of 0.23^[1].
VU6015241 (30 mg/kg; i.p.; single dose) administered intraperitoneally at 30 mg/kg to mice results in moderate brain exposure with a K_p of 0.38, which is higher than the brain exposure observed in rats at the same dose and route^[1].

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

Chemical Information

CAS. Nr. 2264025-00-3
Molecular Weight 449.59
Formel C₂₆H₃₅N₅O₂
SMILES

CC(NC(C=C1)=CC=C1C(N=N2)=CC=C2NC[C@H]3C4(CCN(CC4)CC5CCOCC5)C3)=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]. Bender AM, et al. Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M₄ muscarinic acetylcholine receptor. Bioorg Med Chem Lett. 2022;56:128479. [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.

Keywords

100 mg

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

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VU6015241

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

VU6015241 Related Classifications

HY-182384 Related Classifications