Adoprazine
Based on 1 Customer Validation
Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics.
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- Purity: 98.60%
- CAS No.: 222551-17-9
- 화학식: C24H24FN3O2
- 분자량:405.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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5-HT1A Receptor 9 (pEC50) |
5-HT1A Receptor |
D2 Receptor 9.3 (pA2) |
D3 Receptor 8.9 (pA2) |
D4 Receptor 8.0 (pKi) |
5-HT7 Receptor 7.2 (pKi) |
5-HT1A Receptor 9.1 (pKi) |
D2 Receptor 8.4 (pKi) |
D3 Receptor 8.4 (pKi) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
75.9 μM
Compound: ADOPRAZINE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
18.59 μM
Compound: ADOPRAZINE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
Adoprazine has high affinity at human recombinant D2, D3, D4, 5-HT2B, and 5-HT1A receptors, with pKis of 8.4, 8.4, 8.0, 7.9 and 9.1, respectively[1].
Adoprazine acts as a high potency dopamine D2 receptor antagonist and an efficacious serotonin 5-HT1A receptor agonist, with Emax value (% effect of 10 μM 5-HT) of 73 and pKB value of 8.5 [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (275-350 g) [1]
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Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:p.o.; single
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Result:Led to a dose- and time-dependent increase in extracellular levels of DA, DOPAC, and HVA. In contrast, led to a reduction in 5-HT levels and no change in 5-HIAA levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 222551-17-9
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Appearance Solid
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분자량 405.46
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화학식 C24H24FN3O2
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Color Light yellow to yellow
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SMILES
FC1=CC=C(C2=CN=CC(CN3CCN(C4=C5OCCOC5=CC=C4)CC3)=C2)C=C1
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Synonyms
SLV313
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 50 mg/mL (123.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (7.40 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 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]. Andrew C McCreary, et al. SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. [Content Brief]
[2]. Liesbeth A Bruins Slot, et al. Differential profile of antipsychotics at serotonin 5-HT1A and dopamine D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4663 mL | 12.3317 mL | 24.6633 mL | 61.6584 mL |
| 5 mM | 0.4933 mL | 2.4663 mL | 4.9327 mL | 12.3317 mL | |
| 10 mM | 0.2466 mL | 1.2332 mL | 2.4663 mL | 6.1658 mL | |
| 15 mM | 0.1644 mL | 0.8221 mL | 1.6442 mL | 4.1106 mL | |
| 20 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0829 mL | |
| 25 mM | 0.0987 mL | 0.4933 mL | 0.9865 mL | 2.4663 mL | |
| 30 mM | 0.0822 mL | 0.4111 mL | 0.8221 mL | 2.0553 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5415 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0276 mL | |
| 80 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL |
Adoprazine Related Classifications
HY-14782 Related Classifications
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