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Cat. No.: HY-12501

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ITI-214 free base

Name: ITI-214 free base
Brand: MedChemExpress
SKU: HY-12501
Price: 190.00 USD
Availability: PreOrder

3 Cited Publications

고객리뷰

Based on 3 publication(s) in Google Scholar

ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (K_i 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 K_is of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.0%
CAS No.: 1160521-50-5
화학식: C₂₉H₂₆FN₇O
분자량:507.56

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ITI-214 free base Chemical Structure

CAS No.: 1160521-50-5

사이즈

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재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

PDE1

58 pM (Ki)

PDE1A

33 pM (Ki)

PDE1B

380 pM (Ki)

PDE1C

35 pM (Ki)

All Phosphodiesterase (PDE) Isoforms :

In Vitro

ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (K_i= 34 pM), r-hPDE1B (K_i= 380 pM), and r-hPDE1C (K_i= 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 (K_i= 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. .

In Vivo

ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Sprague-Dawley rats^[1]
Dosage:

0.1-10 mg/kg
Administration:

P.o.
Result:

Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.

Chemical Information

CAS No. 1160521-50-5
Appearance Solid
분자량 507.56
화학식 C₂₉H₂₆FN₇O
Color White to off-white
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
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All ELISAWBIn Vivo Efficacy Study

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Journal Impact Factor

Sci Adv

Transcriptional determinants of lipid mobilization in human adipocytes. [Abstract]

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.
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.
Patent

US20230111925A1.

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).

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

ITI-214 free base

3 Cited Publications

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Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
순도&문서
References

1/16
1/16

ITI-214 free base purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Jan 5;10(1):eadi2689. [Abstract]

Customer Validation
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.
1/16

ITI-214 free base purchased from MedChemExpress. Usage Cited in: Cells. 2023 Dec 3;12(23):2759. [Abstract]

Customer Validation
PDE1 inhibition with ITI-214 (1 μM; 10 min) amplified phospholamban (PLN) phosphorylation at Ser16 upon CNP and SNP stimulation.
1/16

ITI-214 free base purchased from MedChemExpress. Usage Cited in: Patent. US20230111925A1.

Customer Validation
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).

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ITI-214 free base

Publications Citing Use of MedChemExpress (MCE) ITI-214 free base

All Phosphodiesterase (PDE) Isoforms