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Cat. No.: HY-184883

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VU6035406

VU6035406 is a functionally selective mAChR inhibitor, with mAChR IC₅₀ values of 21 nM, 51 nM and 47 nM against human, rat and mouse targets, respectively. VU6035406 does not act as a P-glycoprotein substrate. VU6035406 shows extremely low inhibitory activity against cytochrome P450 1A2, 2C9, 2D6 and 3A4. VU6035406 can be used in the research of neurological and psychiatric disorders.

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CAS No.: 2746405-41-2
Formule: C₁₅H₁₆ClN₅O₃S
Masse moléculaire:381.84

Stockage:

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

VU6035406 Chemical Structure

CAS No.: 2746405-41-2

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target^[1]

mAChR5

21
nM (IC₅₀, human M5 )

mAChR5

51 nM (IC₅₀, rat M5 (rM5)
)

mAChR5

47 nM (IC₅₀, mouse M5 (mM5))

Voir tous les produits spécifiques à Isoform mAChR :

In Vitro

VU6035406 potently inhibits human M₅ muscarinic acetylcholine receptor-mediated calcium mobilization in hM₅ CHO cells with an IC₅₀ of 21 nM and exhibits >500-fold selectivity over human M₁-M₄ subtypes^[1].
VU6035406 inhibits rat M₅ muscarinic acetylcholine receptor-mediated calcium mobilization with an IC₅₀ of 51 nM and exhibits high selectivity over rat M₁-M₄ subtypes^[1].
VU6035406 inhibits mouse M₅ muscarinic acetylcholine receptor-mediated calcium mobilization with an IC₅₀ of 47 nM^[1].
VU6035406 has a favorable CYP inhibition profile, with no significant inhibition of CYP1A2 or CYP2C9 and weak inhibition of CYP2D6 and CYP3A4^[1].
VU6035406 has low to moderate predicted hepatic clearance across multiple species, favorable unbound fractions in plasma and brain, and moderate brain penetration in rats with a K_p,uu of 0.56^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_inf	Bioavailability	T_1/2	MRT	CL	V_ss
Rat^[1]	1.0 mg/kg	i.v.	/	/	524 ng·h/mL	/	1.0 h	1.3 h	31.8 mL/min/kg	2.37 L/kg
Rat^[1]	10 mg/kg	p.o.	1910 ng/mL	2.0 h	13278 ng·h/mL	>100 %	/	/	/	/
Dog^[1]	3.0 mg/kg	p.o.	699 ng/mL	0.58 h	7070 ng·h/mL	58 %	/	/	/	/

Chemical Information

CAS No. 2746405-41-2
Masse moléculaire 381.84
Formule C₁₅H₁₆ClN₅O₃S
SMILES

O=S(C1=CN=C(C)O1)(N2CCC(CC2)C3=CN4N=CN=C4C=C3Cl)=O
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]. Li J, et al. Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M Muscarinic Acetylcholine Receptor. Journal of medicinal chemistry. 2024 Aug 22;67(16):14394-14413. [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.

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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VU6035406

Voir tous les produits spécifiques à Isoform mAChR

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

VU6035406 Related Classifications

HY-184883 Related Classifications

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