1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU0357017 hydrochloride

VU0357017 hydrochloride (Synonyms: CID-25010775)

Cat. No.: HY-19752A Purity: 99.28%
Handling Instructions

VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.

For research use only. We do not sell to patients.

VU0357017 hydrochloride Chemical Structure

VU0357017 hydrochloride Chemical Structure

CAS No. : 1135242-13-5

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 144 In-stock
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50 mg USD 540 In-stock
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100 mg USD 960 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia[1][2][3].

IC50 & Target

IC50: 477 nM (M1)[1]

In Vitro

VU0357017 is selective for M1 (Ki=9.91 µM) over M2-M5 mAChRs (Ki=21.4, 55.3, 35.0, and 50.0 μM, respectively) in CHO cells[1].
VU0357017 (1 nM-100 μM) induces calcium release and ERK phosphorylation in a concentration-dependent manner in CHO cells[3].

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

In Vivo

VU0357017 (1-10 mg/kg, i.p.) reverses scopolamine-induced disruption of the contextual fear conditioning response[2].

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

Animal Model: Male Sprague−Dawley rats (380-420 g) were pretreated with scopolamine[2]
Dosage: 1, 3, 10 mg/kg
Administration: A single i.p.
Result: Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg.
Molecular Weight

369.89

Formula

C₁₈H₂₈ClN₃O₃

CAS No.
SMILES

O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (67.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7035 mL 13.5175 mL 27.0351 mL
5 mM 0.5407 mL 2.7035 mL 5.4070 mL
10 mM 0.2704 mL 1.3518 mL 2.7035 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.76 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.76 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VU0357017CID-25010775VU 0357017VU-0357017CID25010775CID 25010775mAChRMuscarinic acetylcholine receptorM1muscarinicacetylcholine,Alzheimer’sschizophreniaInhibitorinhibitorinhibit

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Product Name:
VU0357017 hydrochloride
Cat. No.:
HY-19752A
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