1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. VU0364572 TFA

VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant.

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VU0364572 TFA Chemical Structure

VU0364572 TFA Chemical Structure

CAS No. : 1240514-89-9

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Based on 1 publication(s) in Google Scholar

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Description

VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant[1][3].

IC50 & Target[3]

mAChR1

0.11 μM (EC50)

In Vitro

VU0364572 (30 μM; 25 min) TFA promotes KCNQ2, NR1 and MARCKS phosphorylation in striatal/NAc slices[2].

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

Western Blot Analysis[2]

Cell Line: Striatal/NAc slices
Concentration: 30 μM
Incubation Time: 25 min
Result: Significantly increased the phosphorylation of KCNQ2 at T217, NR1 at S890, and MARCKS at S152/156.
In Vivo

VU0364572 (10 mg/kg/day; oral; 4 months) TFA shows neuroprotective effects in 5XFAD transgenic Alzheimer’s mice. VU0364572 has a half life of 45 minutes[1].

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

Animal Model: 5XFAD transgenic Alzheimer’s mice[1]
Dosage: 10 mg/kg/day
Administration: In drinking water, from 2 months of age to 6 months
Result: Preserved hippocampal memory. Significantly reduced levels of soluble and insoluble Aβ40,42 in the cortex and hippocampus of these animals. Significantly decreased oligomeric (oAβ) levels in the cortex.
Molecular Weight

487.51

Formula

C23H32F3N3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC(N2C[C@H](NC(C3=CC=CC=C3C)=O)CCC2)CC1)OCC.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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VU0364572 TFA Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
VU0364572 TFA
Cat. No.:
HY-113616A
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