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Purity: ≥98%
Pardoprunox (formerly known as SLV-308, DU-126891 or SME-308) is novel & potent dopamine D2/5-HT1A receptor agonist that has the potential for the treatment of Parkinson's disease. Pardoprunox functions by binding to 5-HT(1) (A) and dopamine D(2), D(3), and D(4) receptors.It is a full agonist at serotonin 5-HT(1) (A) receptors and a partial agonist at dopamine D(2) and D(3) receptors. SLV308 functioned as a strong but partial D(2) receptor agonist at cloned human dopamine D(2,L) receptors (pEC(50) = 8.0 and pA(2) = 8.4) with a 50% efficacy on forskolin stimulated cAMP accumulation. SLV308 functioned as a partial agonist at human recombinant dopamine D(3) receptors, inducing [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and inhibiting the dopamine-induced [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 had low potency (pEC(50) = 6.3) but nonetheless functioned as a complete 5-HT(1) (A) receptor agonist on forskolin-induced cAMP accumulation at cloned human 5-HT(1) (A) receptors.
| Targets |
5-HT1A Receptor ( pEC50 = 6.3 ); D2 Receptor ( pEC50 = 8 ); D3 Receptor ( pEC50 = 9.2 nM )
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| ln Vitro |
Pardoprunox (SLV-308) hydrochloride has a 50% efficacy on forskolin-stimulated cAMP accumulation and functions as a strong but partial D2 receptor agonist (pEC50= 8.0 and pA2= 8.4). Pardoprunox hydrochloride antagonizes the dopamine-induced [(35)S]GTPgammaS binding (pA2=9.0) and functions as a partial agonist at human recombinant dopamine D3 receptors, inducing [(35)S]GTPgammaS binding with an intrinsic activity of 67%. On forskolin-induced cAMP accumulation at cloned human 5-HT1A receptors, pardoprunox hydrochloride functions as a full 5-HT1A receptor agonist, albeit with low potency (pEC50=6.3)[1].
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| ln Vivo |
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| Enzyme Assay |
Pardoprunox also exhibits a lower affinity for binding to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2). With a 50% efficacy on forskolin-stimulated cAMP accumulation, pardoprunox exerts a strong but partial D(2) receptor agonist (pEC50 = 8.0 and pA2 = 8.4). Pardoprunox inhibits the dopamine-induced induction of [35S]GTPgammaS binding (pA2 = 9.0) and functions as a partial agonist at human recombinant dopamine D3 receptors, where it induces [35S]GTPgammaS binding with an intrinsic activity of 67%. While cloned human 5-HT1A receptors are induced to accumulate cAMP by forskolin, pardoprunox functions as a full 5-HT1A receptor agonist with a low potency (pEC50 = 6.3).
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| References |
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| Molecular Formula |
C12H16CLN3O2
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| Molecular Weight |
269.73
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| Exact Mass |
269.09
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| Elemental Analysis |
C, 53.44; H, 5.98; Cl, 13.14; N, 15.58; O, 11.86
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| CAS # |
269718-83-4
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| Related CAS # |
Pardoprunox; 269718-84-5
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| Appearance |
Pale mauve solid powder
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| SMILES |
CN1CCN(CC1)C2=CC=CC3=C2OC(=O)N3.Cl
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| InChi Key |
NQRIKTDKFHAOKC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H15N3O2.ClH/c1-14-5-7-15(8-6-14)10-4-2-3-9-11(10)17-12(16)13-9;/h2-4H,5-8H2,1H3,(H,13,16);1H
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| Chemical Name |
7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 30~150 mg/mL (111.2~556.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (27.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 7.5 mg/mL (27.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 7.5 mg/mL (27.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7074 mL | 18.5371 mL | 37.0741 mL | |
| 5 mM | 0.7415 mL | 3.7074 mL | 7.4148 mL | |
| 10 mM | 0.3707 mL | 1.8537 mL | 3.7074 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00903838 | Terminated | Drug: pardoprunox | Advanced Stage Parkinson's Disease | Abbott Products | September 2009 | Phase 2 |
| NCT00335374 | Completed | Drug: Pardoprunox | Early Stage Parkinson's Disease | Solvay Pharmaceuticals | August 2007 | Phase 3 |
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