country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-12501

Copy Link Print Information

ITI-214 free base

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

3 Cited Publications

カスタマーレビュー

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度 : 98.0%
CAS 番号: 1160521-50-5
分子式: C₂₉H₂₆FN₇O
分子量:507.56

保管条件:

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

ITI-214 free base 構造式

CAS 番号: 1160521-50-5

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (3)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

PDE1

58 pM (Ki)

PDE1A

33 pM (Ki)

PDE1B

380 pM (Ki)

PDE1C

35 pM (Ki)

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

CAS 番号 1160521-50-5
性状 Solid
分子量 507.56
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Sort by:

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).

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

100 mg お問い合わせ

Subscribe to the

MedChemExpress

Newsletter

MOQ

Minimum order quantity

100 mg

お問い合わせ在庫あり

Other size

お問い合わせ

Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (3)
純度とドキュメンテーション
参考文献

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).

製品名:
製品番号:
数量:
日本の代理先をお選びください:

製品名:
CAS 番号:
生物種:
純度:
数量:

ITI-214 free base

MedChemExpress（MCE）の使用を引用している文献 ITI-214 free base

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC₅₀ & Target

体外実験

体内実験

化学情報

Publications (3)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Bioz

Keywords

最近チェックした製品

ITI-214 free base

MedChemExpress（MCE）の使用を引用している文献 ITI-214 free base

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

体内実験

化学情報

Publications (3)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

ITI-214 free base 関連分類

HY-12501 関連分類

Bioz

Keywords

最近チェックした製品

IC₅₀ & Target