1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    5-HT Receptor
    Arrestin
  3. UNC9994 hydrochloride

UNC9994 hydrochloride 

Cat. No.: HY-111385 Purity: 98.83%
COA Handling Instructions

UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.

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

UNC9994 hydrochloride Chemical Structure

UNC9994 hydrochloride Chemical Structure

CAS No. : 2108826-33-9

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Based on 1 publication(s) in Google Scholar

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Description

UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity[1].

IC50 & Target

D3 Receptor

17 nM (Ki)

D2 Receptor

79 nM (Ki)

D4 Receptor

138 nM (Ki)

D1 Receptor

4000 nM (Ki)

5-HT2B Receptor

25 nM (Ki)

5-HT1A Receptor

26 nM (Ki)

5-HT2A Receptor

140 nM (Ki)

5-HT2C Receptor

512 nM (Ki)

In Vitro

UNC9994 hydrochloride induces D2-mediated β-arrestin-2 translocation with an EC50s of 6.1 nM and 448 nM in Tango assay and DiscoveRx assay, respectively[1].
UNC9994 hydrochloride is an antagonist at 5HT2A and 5HT2B and an agonist at 5HT2C and 5HT1A[1].

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

In Vivo

UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice[1].

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

Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice[1]
Dosage: 2.0 mg/kg, followed 30 min later with 6 mg/kg phencyclidine (PCP, i.p.)
Administration: IP, once
Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice and the activity was completely abolished in β-arrestin-2 knockout mice.
Molecular Weight

457.84

Appearance

Solid

Formula

C21H23Cl3N2OS

CAS No.
SMILES

ClC1=C(Cl)C(C2CCN(CCCOC3=CC=C(SC=N4)C4=C3)CC2)=CC=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 98.83%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
UNC9994 hydrochloride
Cat. No.:
HY-111385
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