ITI-214 free base
Based on 3 publication(s) in Google Scholar
ITI-214 free base 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 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1160521-50-5
- Formula: C29H26FN7O
- Molecular Weight:507.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ITI-214 free base
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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
Biological Activity
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PDE1 58 pM (Ki) |
PDE1A 33 pM (Ki) |
PDE1B 380 pM (Ki) |
PDE1C 35 pM (Ki) |
ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (Ki= 34 pM), r-hPDE1B (Ki= 380 pM), and r-hPDE1C (Ki= 37 pM) enzymes transiently expressed in HEK cells. The compound expressed >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.
Chemical Information
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CAS No. 1160521-50-5
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Appearance Solid
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Molecular Weight 507.56
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Formula C29H26FN7O
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 free base 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 free base 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 free base 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).
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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 Feb 11;59(3):1149-64. [Content Brief]
[2]. Lawrence Wennogle. Novel uses. From PCT Int. Appl. (2014), WO 2014145617 A2 20140918.
[3]. Peng Li , et al. Salt crystals. From PCT Int. Appl. (2013), WO 2013192556 A2 20131227.
[4]. Allen A. Fienberg, et al. Organic compounds. From PCT Int. Appl. (2010), WO 2010132127 A1 20101118.
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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