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Referencia número: 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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No. CAS: 2264025-00-3
Fòrmula: C₂₆H₃₅N₅O₂
Peso molecular:449.59

Almacenamiento:

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

VU6015241 Chemical Structure

No. CAS: 2264025-00-3

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
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Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas mAChR :

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

No. CAS 2264025-00-3
Peso molecular 449.59
Fòrmula C₂₆H₃₅N₅O₂
SMILES

CC(NC(C=C1)=CC=C1C(N=N2)=CC=C2NC[C@H]3C4(CCN(CC4)CC5CCOCC5)C3)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

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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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100 mg

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- In Vitro
- In Vivo
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VU6015241

Ver todos los productos específicos de isoformas mAChR

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

VU6015241 Related Classifications

HY-182384 Related Classifications