UNC9994
Based on 3 publication(s) in Google Scholar
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
For research use only. We do not sell to patients.
- Purity : 98.06%
- CAS No.: 1354030-51-5
- Formula: C21H22Cl2N2OS
- Molecular Weight:421.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) UNC9994
MoreAll Dopamine Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
D2 Receptor 79 nM (Ki) |
D3 Receptor 17 nM (Ki) |
D4 Receptor 138 nM (Ki) |
5-HT2A Receptor 140 nM (Ki) |
5-HT2B Receptor 25 nM (Ki) |
5-HT2C Receptor 512 nM (Ki) |
5-HT1F Receptor 26 nM (Ki) |
H1 Receptor 2.1 nM (Ki) |
In Vitro
UNC9994 displays a lower binding affinity (Ki=79 nM) to D2R than UNC9975, UNC0006, and aripiprazole. At serotonin (as known as 5-HT) receptors, UNC9994 displays moderate to high binding affinities (Ki=25-512 nM) for 5HT2A, 5HT2B, 5HT2C, and 5HT1A, but is significantly less potent in functional assays (Ca2+ mobilization FLIPR or cAMP biosensor). UNC9994 is an antagonist at 5HT2A and 5HT2B and agonists at 5HT2C and 5HT1A. UNC9994 has relatively high affinities to H1-histamine receptor (Ki=2.4 nM) but is less potent antagonists in H1 functional assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)[1]
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Dosage:2 mg/kg
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Administration:I.p. followed 30 min later with 6 mg/kg phencyclidine
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Result:Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
Chemical Information
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CAS No. 1354030-51-5
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Appearance Solid
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Molecular Weight 421.38
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Formula C21H22Cl2N2OS
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Color White to off-white
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SMILES
ClC1=CC=CC(C2CCN(CC2)CCCOC3=CC4=C(C=C3)SC=N4)=C1Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Theranostics
Morphine- and foot shock-responsive neuronal ensembles in the VTA possess different connectivity and biased GPCR signaling pathway. [Abstract]2024 Jan 12;14(3):1126-1146. PMID: 38250036 -
Acta Pharmacol Sin
G protein-dependent dopamine D2 receptor signaling mediates cocaine-primed reinstatement. [Abstract]2026 Jan 14. PMID: 41535707 -
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UNC9994 Related Classifications
HY-117829 Related Classifications
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