1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR

VU0357017 hydrochloride (Synonyms: CID-25010775)

Cat. No.: HY-19752A Purity: 99.89%
Handling Instructions

VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15). IC50 value: 477 ± 172 nM (EC50) [1] Target: M1 in vitro: VU0357017 is a M1-selective agonists that appear to activate M1 through actions at an allosteric site. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. [1] VU0357017 is a potent and efficacious M1 agonist, selective versus M2 M5 family members and allosteric agonist. VU0357017 is a highly selective M1 agonist suggests that these compounds are unlikely to act at the highly conserved orthosteric site on M1 and are more likely to act as allosteric agonists. [2] VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 significantly enhances threshold Θ-burst LTP and VU0364572 induces LTD at the Schaffer collateral-CA1 synapse of rodent hippocampal slices. [3] in vivo: VU0357017 has robust efficacy in improving hippocampal-dependent learning in rats. VU0357017 enhances performance in Morris water maze and contextual fear conditioning in rats. [3]

Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (89.22 mM)

*"≥" means soluble, but saturation unknown.

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.
References
Molecular Weight

369.89

Formula

C₁₈H₂₈ClN₃O₃

CAS No.

1135242-13-5

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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

Cat. No.: HY-19752A