ITI-214
Based on 3 publication(s) in Google Scholar
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.56%
- No. CAS: 1642303-38-5
- Fòrmula: C29H29FN7O5P
- Peso molecular:605.56
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) ITI-214
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Customer Validation & Images
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ELISA
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WB
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In Vivo Efficacy Study
Actividad biológica
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PDE1 58 pM (Ki) |
PDE1A 33 pM (Ki) |
PDE1B 380 pM (Ki) |
PDE1C 35 pM (Ki) |
ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki= 33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families[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 Sprague-Dawley rats[1]
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Dosage:0.1-10 mg/kg
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Administration:p.o.
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Result:Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1642303-38-5
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Appearance Solid
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Peso molecular 605.56
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Fòrmula C29H29FN7O5P
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Color White to off-white
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SMILES
O=C(C1=C(NC2=CC=CC=C2)N(CC3=CC=C(C4=NC(F)=CC=C4)C=C3)N=C1N56)N(C)C5=N[C@@]7([H])[C@]6([H])CCC7.O=P(O)(O)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Adv
2024 Jan 5;10(1):eadi2689. PMID: 38170777
ITI-214 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Jan 5;10(1):eadi2689. [Abstract]
Effects of the PDE1 inhibitor ITI-214 (1 μM; 1 h pre-incubation followed by 20 min ANP stimulation in the continued presence of ITI-214) on ANP-stimulated cGMP levels in untransfected or siC versus siZ adipocytes. ITI-214 increased cGMP levels and eliminated the difference in cGMP levels between ZNF189-depleted and control cells.
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Cells
Role of Phosphodiesterase 1 in the Regulation of Real-Time cGMP Levels and Contractility in Adult Mouse Cardiomyocytes. [Abstract]2023 Dec 3;12(23):2759. PMID: 38067187
ITI-214 purchased from MedChemExpress. Usage Cited in: Cells. 2023 Dec 3;12(23):2759. [Abstract]
PDE1 inhibition with ITI-214 (1 μM; 10 min) amplified phospholamban (PLN) phosphorylation at Ser16 upon CNP and SNP stimulation.
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ITI-214 purchased from MedChemExpress. Usage Cited in: Patent. US20230111925A1.
Body-weight changes, survival rates, colon lengths, and disease activity index (DAI) scores in 2% DSS-induced C57BL/6 mice administered ITI-214 (PDE1i; 3 mg/kg; i.p.; twice daily on days 4-8).
Solvente y solubilidad
DMSO : 100 mg/mL (165.14 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, 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.
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.
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: ≥ 2.5 mg/mL (4.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li P, et al. Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem. 2016;59(3):1149-1164. [Content Brief]
[2]. Snyder GL, et al. Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats. Psychopharmacology (Berl). 2016;233(17):3113-3124. [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 |
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| DMSO | 1 mM | 1.6514 mL | 8.2568 mL | 16.5136 mL | 41.2841 mL |
| 5 mM | 0.3303 mL | 1.6514 mL | 3.3027 mL | 8.2568 mL | |
| 10 mM | 0.1651 mL | 0.8257 mL | 1.6514 mL | 4.1284 mL | |
| 15 mM | 0.1101 mL | 0.5505 mL | 1.1009 mL | 2.7523 mL | |
| 20 mM | 0.0826 mL | 0.4128 mL | 0.8257 mL | 2.0642 mL | |
| 25 mM | 0.0661 mL | 0.3303 mL | 0.6605 mL | 1.6514 mL | |
| 30 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3761 mL | |
| 40 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0321 mL | |
| 50 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL | |
| 60 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6881 mL | |
| 80 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5161 mL | |
| 100 mM | 0.0165 mL | 0.0826 mL | 0.1651 mL | 0.4128 mL |
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