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VU0152100

Catalog No. T17238   CAS 409351-28-6
Synonyms: VU152100

VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).

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VU0152100 Chemical Structure
VU0152100, CAS 409351-28-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 81.00
10 mg In stock $ 121.00
25 mg In stock $ 267.00
50 mg In stock $ 519.00
100 mg In stock $ 779.00
200 mg In stock $ 1,090.00
500 mg In stock $ 1,650.00
1 mL * 10 mM (in DMSO) In stock $ 100.00
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Purity: 99.43%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).
In vitro VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1].
In vivo Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1].
Synonyms VU152100
Molecular Weight 341.43
Formula C18H19N3O2S
CAS No. 409351-28-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (131.80 mM)

TargetMolReferences and Literature

1. Brady AE, et al. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library NO PAINS Compound Library Anti-Parkinson's Disease Compound Library Anti-Alzheimer's Disease Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

VU0152100 409351-28-6 Neuroscience AChR VU 152100 VU 0152100 Inhibitor VU152100 Muscarinic acetylcholine receptor inhibit mAChR VU-152100 VU-0152100 inhibitor

 

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