1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. ITI214

ITI214 

製品番号: HY-12501A 純度: 99.58%
取扱説明書

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

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ITI214 構造式

ITI214 構造式

CAS 番号 : 1642303-38-5

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 560 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 600 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1800 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2520 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). IC50 value: 58 pM (Ki) Target: PDE1 in vitro: ITI-214 exhibits picomolar inhibitory potency for PDE1, demonstrates excellent selectivity against all other PDE families. ITI214 exhibits excellent selectivity over other PDE family members. For instance, the Ki values of ITI214 against recombinant full-length human PDE1A, PDE1B, and PDE1C are 33 pM, 380 pM, and 35 pM, respectively. ITI214 is profiled in a panel of enzymes, receptors, transporters, and ion channels from Caliper at 10 μM, which is over 170000 times higher than its Ki for PDE1, and demonstrates good selectivity. [1] in vivo: ITI214 possesses a good overall profile with balanced physicochemical properties, excellent potency and selectivity, and good pharmacokinetics. ITI214 is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg. [1]

臨床実験
分子量

605.56

分子式

C₂₉H₂₉FN₇O₅P

CAS 番号

1642303-38-5

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[[email protected]@]7([H])[[email protected]]6([H])CCC7.O=P(O)(O)O

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
溶剤 & 溶解度
体外: 

DMSO : ≥ 30 mg/mL (49.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6514 mL 8.2568 mL 16.5136 mL
5 mM 0.3303 mL 1.6514 mL 3.3027 mL
10 mM 0.1651 mL 0.8257 mL 1.6514 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.58%

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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

ITI214ITI 214ITI-214Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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Inquiry Information

製品名:
ITI214
製品番号:
HY-12501A
数量:
MCE 日本正規代理店: