U-99194 maleate
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.23%
- CAS No.: 234757-41-6
- Formula: C21H31NO6
- Molecular Weight:393.47
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Dopamine Receptor Isoforms
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Biological Activity
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D3 Receptor 160 nM (Ki) |
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.
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.
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Animal Model:Nicotine (1 mg/kg, i.p.) was injected to induce kinetic tremor in male ddY mice (7-11 weeks of age)[1]
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Dosage:30 mg/kg
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Administration:i.p., once
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Result:Suppressed Nicotine (HY-127019)-induced tremor.
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Animal Model:Nicotine (1 mg/kg, i.p.) was injected to induce kinetic tremor in Male SD rats (7-11 weeks of age)[1]
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Dosage:30 μg/site
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Administration:intracerebellar microinjection, once
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Result:Suppressed Nicotine (HY-127019)-induced tremor.
Chemical Information
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CAS No. 234757-41-6
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Appearance Solid
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Molecular Weight 393.47
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Formula C21H31NO6
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Color Off-white to light yellow
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SMILES
CCCN(CCC)C1CC2=C(C=C(OC)C(OC)=C2)C1.O=C(O)/C=C\C(O)=O
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Synonyms
U-99194A; PNU-99194A maleate; JPC-211 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kato M, et al. Mechanisms Underlying Dopaminergic Regulation of Nicotine-Induced Kinetic Tremor. Front Pharmacol. 2022 Jun 16;13:938175. [Content Brief]
[2]. Hammad H, et al. Dopamine-mediated disinhibition in the CA1 region of rat hippocampus via D3 receptor activation. J Pharmacol Exp Ther. 2006 Jan;316(1):113-20. [Content Brief]
[3]. Audinot V, et al. A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D3 receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. J Pharmacol Exp Ther. 1998 Oct;287(1):187-97. [Content Brief]
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.