VU0415248
VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1359087-83-4
- Formel: C21H23N5O3S
- Molecular Weight:425.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
mAChR1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.18 μM
Compound: 13l, VU0415248
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Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay
Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay
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[PMID: 22197142] |
In Vitro
VU0415248 inhibits acetylcholine-induced calcium mobilization in human M1 muscarinic acetylcholine receptor-expressing cells with an IC50 of 0.4 μM[1].
VU0415248 (30 μM) inhibits acetylcholine-induced calcium mobilization in rat M1 muscarinic acetylcholine receptor-expressing cells with an IC50 of 0.18 μM, and shows very high selectivity over rat and human M2-5 muscarinic acetylcholine receptors (human M2-5 IC50 > 30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 1359087-83-4
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Molecular Weight 425.50
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Formel C21H23N5O3S
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SMILES
O=C(CCNS(=O)(C1=CC=CC2=NC=CC=C21)=O)N3CCN(CC3)C4=CC=NC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
VU0415248 Related Classifications
HY-182587 Related Classifications
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Keywords
- VU0415248
- 1359087-83-4
- VU 0415248
- VU-0415248
- mAChR
- human M1 muscarinic acetylcholine receptor-expressing cells
- acetylcholine-induced calcium mobilization
- M1
- muscarinic acetylcholine receptor 1
- rat M1 muscarinic acetylcholine receptor-expressing cells
- fragile x syndrome
- parkinson’s disease
- human M2-M5 muscarinic receptor subtypes
- movement disorders
- rat M2-M5 muscarinic receptor subtypes
- Inhibitor
- inhibitor
- inhibit