1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. U-99194 maleate

U-99194 maleate  (Synonyms: U-99194A; PNU-99194A maleate; JPC-211 maleate)

Cat. No.: HY-12701A Pureza: 99.23%
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U-99194 (PNU-99194) maleate is a selective, potent dopamine D3 receptor antagonist (Ki =160 nM). U-99194 maleate inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 maleate abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 maleate can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors.

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U-99194 maleate

U-99194 maleate Estructura química

No. CAS : 234757-41-6

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200 mg   Obtener un presupuesto  

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Based on 1 publication(s) in Google Scholar

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Descripciòn

U-99194 (PNU-99194) maleate is a selective, potent dopamine D3 receptor antagonist (Ki =160 nM). U-99194 maleate inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 maleate abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 maleate can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors[1][2].

IC50 & Target[1]

D3 Receptor

160 nM (Ki)

In Vitro

U-99194 (1 μM, 15 min) maleate prevents the cocaine-induced inhibition of monosynaptic inhibitory postsynaptic currents (IPSCs) evoked from stratum radiatum in CA1 pyramidal neurons of rat hippocampal slices[2].
U-99194 (1 μM) maleate blocks the inhibitory effect of PD 128907 ( HY-100539) on the amplitude of monosynaptic IPSCs evoked from stratum radiatum in CA1 pyramidal neurons of rat hippocampal slices[2].

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

In Vivo

U-99194 (30 mg/kg, i.p., once) maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice[1].
U-99194 (30 μg/site, intracerebellar microinjection, once) maleate markedly inhibits Nicotine-induced tremor in rats[1].

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

Animal Model: Nicotine (1 mg/kg, i.p.) was injected to induce kinetic tremor in male ddY mice (7-11 weeks of age)[1]
Dosage: 30 mg/kg
Administration: i.p., once
Result: Suppressed Nicotine (HY-127019)-induced tremor.
Animal Model: Nicotine (1 mg/kg, i.p.) was injected to induce kinetic tremor in Male SD rats (7-11 weeks of age)[1]
Dosage: 30 μg/site
Administration: intracerebellar microinjection, once
Result: Suppressed Nicotine (HY-127019)-induced tremor.
Peso molecular

393.47

Fòrmula

C21H31NO6

No. CAS
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCCN(CCC)C1CC2=C(C=C(OC)C(OC)=C2)C1.O=C(O)/C=C\C(O)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad
In Vitro: 

DMSO : 125 mg/mL (317.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (50.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5415 mL 12.7074 mL 25.4149 mL
5 mM 0.5083 mL 2.5415 mL 5.0830 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.5415 mL 12.7074 mL 25.4149 mL 63.5372 mL
5 mM 0.5083 mL 2.5415 mL 5.0830 mL 12.7074 mL
10 mM 0.2541 mL 1.2707 mL 2.5415 mL 6.3537 mL
15 mM 0.1694 mL 0.8472 mL 1.6943 mL 4.2358 mL
20 mM 0.1271 mL 0.6354 mL 1.2707 mL 3.1769 mL
25 mM 0.1017 mL 0.5083 mL 1.0166 mL 2.5415 mL
30 mM 0.0847 mL 0.4236 mL 0.8472 mL 2.1179 mL
40 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5884 mL
50 mM 0.0508 mL 0.2541 mL 0.5083 mL 1.2707 mL
DMSO 60 mM 0.0424 mL 0.2118 mL 0.4236 mL 1.0590 mL
80 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7942 mL
100 mM 0.0254 mL 0.1271 mL 0.2541 mL 0.6354 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Nombre del producto:
U-99194 maleate
Cat. No.:
HY-12701A
Cantidad:
MCE Japan Authorized Agent: