1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor 5-HT Receptor
  3. Lumateperone

Lumateperone  (Synonyms: ITI-007)

製品番号: HY-17637 純度: 99.83%
COA 取扱説明書 Technical Support

Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression.

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Lumateperone

Lumateperone 構造式

CAS 番号 : 313368-91-1

容量 価格(税別) 在庫状況 数量
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Oil
5 mg $25 在庫あり
10 mg $40 在庫あり
50 mg $75 在庫あり
100 mg $110 在庫あり
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500 mg   お問い合わせ  

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製品説明

Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression[1][2][3].

IC50 & Target

D1 Receptor

 

D2 Receptor

 

5-HT2A Receptor

 

体外実験

Lumateperone (2-30 μM) has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: RPMI-8226 cells
Concentration: 2-30 μM
Incubation Time: 48 hours
Result: Inhibited cell growth with the IC50 value of 17.30 μM.
体内実験

Lumateperone (i.p., 1-10 mg/kg) promotes NMDA and AMPA-induced currents in a dopamine D1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices[2].

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

Animal Model: Adult male Sprague-Dawley rats[2]
Dosage: 1-10 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes.
Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.
分子量

393.50

分子式

C24H28FN3O

CAS 番号
Appearance

Oil

Color

Light yellow to yellow

SMILES

CN1C2=C3C([C@@]4([H])[C@@](CCN(C4)CCCC(C5=CC=C(C=C5)F)=O)([H])N3CC1)=CC=C2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (254.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5413 mL 12.7065 mL 25.4130 mL
5 mM 0.5083 mL 2.5413 mL 5.0826 mL
10 mM 0.2541 mL 1.2706 mL 2.5413 mL
View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます:C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 99.83%

参考文献

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 (protect from light). 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
DMSO 1 mM 2.5413 mL 12.7065 mL 25.4130 mL 63.5324 mL
5 mM 0.5083 mL 2.5413 mL 5.0826 mL 12.7065 mL
10 mM 0.2541 mL 1.2706 mL 2.5413 mL 6.3532 mL
15 mM 0.1694 mL 0.8471 mL 1.6942 mL 4.2355 mL
20 mM 0.1271 mL 0.6353 mL 1.2706 mL 3.1766 mL
25 mM 0.1017 mL 0.5083 mL 1.0165 mL 2.5413 mL
30 mM 0.0847 mL 0.4235 mL 0.8471 mL 2.1177 mL
40 mM 0.0635 mL 0.3177 mL 0.6353 mL 1.5883 mL
50 mM 0.0508 mL 0.2541 mL 0.5083 mL 1.2706 mL
60 mM 0.0424 mL 0.2118 mL 0.4235 mL 1.0589 mL
80 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7942 mL
100 mM 0.0254 mL 0.1271 mL 0.2541 mL 0.6353 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Lumateperone
製品番号:
HY-17637
数量:
MCE 日本正規代理店: