LY3154207
Based on 2 publication(s) in Google Scholar
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
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- Pureté: 98.06%
- CAS No.: 1638667-79-4
- Formule: C24H29Cl2NO3
- Masse moléculaire:450.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LY3154207
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Activité biologique
EC50: 3 nM (human dopamine D1 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1.11 nM
Compound: 35; LY3154207
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Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
| HEK293 | EC50 |
12.8 nM
Compound: 3; LY3154207
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Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assay
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
2 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at dog D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at dog D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
2.3 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
2.5 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at rhesus monkey D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at rhesus monkey D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
3 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
62.1 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
>10000 nM
Compound: 3; LY3154207
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Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
In HEK293 cells transiently expressing human, dog, rhesus monkey, and mouse D1 receptors, the EC50s of LY3154207 are 2.3 nM, 2.0 nM, 2.5 nM, and 62.1 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1638667-79-4
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Appearance Solid
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Masse moléculaire 450.40
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Formule C24H29Cl2NO3
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Color White to off-white
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SMILES
O=C(N1[C@@H](C)C2=C(C(CCC(C)(O)C)=CC=C2)C[C@@H]1CO)CC3=C(Cl)C=CC=C3Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2022 Jun 8;13(1):3186. PMID: 35676276 -
Solvant et solubilité
DMSO : 110 mg/mL (244.23 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: ≥ 2.75 mg/mL (6.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.2202 mL | 11.1012 mL | 22.2025 mL | 55.5062 mL |
| 5 mM | 0.4440 mL | 2.2202 mL | 4.4405 mL | 11.1012 mL | |
| 10 mM | 0.2220 mL | 1.1101 mL | 2.2202 mL | 5.5506 mL | |
| 15 mM | 0.1480 mL | 0.7401 mL | 1.4802 mL | 3.7004 mL | |
| 20 mM | 0.1110 mL | 0.5551 mL | 1.1101 mL | 2.7753 mL | |
| 25 mM | 0.0888 mL | 0.4440 mL | 0.8881 mL | 2.2202 mL | |
| 30 mM | 0.0740 mL | 0.3700 mL | 0.7401 mL | 1.8502 mL | |
| 40 mM | 0.0555 mL | 0.2775 mL | 0.5551 mL | 1.3877 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1101 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9251 mL | |
| 80 mM | 0.0278 mL | 0.1388 mL | 0.2775 mL | 0.6938 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5551 mL |
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