製品番号: HY-132981

Lu AF27139

Name: Lu AF27139
Brand: MedChemExpress
SKU: HY-132981
Price: 270.00 USD
Availability: InStock
Rating: 5 (1 reviews)

カスタマーレビュー

Based on 1 Customer Validation

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC₅₀s of 12 and 2.4 nM for human and rat, K_is of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.

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 : 99.71%
CAS 番号: 2097117-06-9
分子式: C₂₁H₁₉ClF₃N₅O₂S
分子量:497.92

保管条件:

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

Lu AF27139 構造式

CAS 番号: 2097117-06-9

容量

価格（税別）

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数量

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

P2X7 Receptor

P2X Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Microglia	IC₅₀	26 nM Compound: 1; Lu AF27139	Inhibition of BzATP-induced IL-1beta in mouse primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader Inhibition of BzATP-induced IL-1beta in mouse primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader	[PMID: 33822617]
Microglia	IC₅₀	38 nM Compound: 1; Lu AF27139	Inhibition of BzATP-induced IL-1beta in rat primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader Inhibition of BzATP-induced IL-1beta in rat primary microglia cells primed with LPS measured after repeated BzATP treatment by microplate reader	[PMID: 33822617]
THP-1	IC₅₀	38 nM Compound: 1; Lu AF27139	Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader	[PMID: 33822617]

体外実験

Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC₅₀ of 66 nM^[1].
Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose^[1].
Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC₅₀ of 38 ± 2.5 nM^[1].
Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice^[1].

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

体内実験

Lu AF27139 (compound 1) (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice^[1].
Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat^[1].

dose	C_{u, plasma} (nM)^a		C_{u, brain} (nM)^a		C_{u, spinal cord} (nM)^a
(mg/kg, po)	(1 h)	(2 h)	(1 h)	(2 h)	(1 h)	(2 h)
T₁	22.4 ± 4.2	22.8 ± 10	5.4 ± 2.6	6.4 ± 2.0	5.20 ± 0.80	10.0 ± 2.0

a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*f_u), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and f_u is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. f_u, plasma = 0.02 ± 0.00, f_u, spinal cord = 0.07 ± 0.03, and f_u, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.

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

Animal Model:

Male Sprague−Dawley rats (280−350 g); Male C57BL mice (18−25g)^[1]
Dosage:

3, 10, and 100 mg/kg
Administration:

p.o.
Result:

Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.

化学情報

CAS 番号 2097117-06-9
性状 Solid
分子量 497.92
分子式 C₂₁H₁₉ClF₃N₅O₂S
Color White to off-white
SMILES

ClC(C=C1)=CC=C1[C@H](N2CCOCC2)CNC(C3=C(C(F)(F)F)N=C(C4=NC=CC=N4)S3)=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 : 125 mg/mL (251.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0084 mL

10.0418 mL

20.0835 mL

5 mM

0.4017 mL

2.0084 mL

4.0167 mL

10 mM

0.2008 mL

1.0042 mL

2.0084 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

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 (276 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]. Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021 Apr 22;64(8):4891-4902. [Content Brief]

[2]. Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021;64(8):4891-4902.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.0084 mL	10.0418 mL	20.0835 mL	50.2089 mL
	5 mM	0.4017 mL	2.0084 mL	4.0167 mL	10.0418 mL
	10 mM	0.2008 mL	1.0042 mL	2.0084 mL	5.0209 mL
	15 mM	0.1339 mL	0.6695 mL	1.3389 mL	3.3473 mL
	20 mM	0.1004 mL	0.5021 mL	1.0042 mL	2.5104 mL
	25 mM	0.0803 mL	0.4017 mL	0.8033 mL	2.0084 mL
	30 mM	0.0669 mL	0.3347 mL	0.6695 mL	1.6736 mL
	40 mM	0.0502 mL	0.2510 mL	0.5021 mL	1.2552 mL
	50 mM	0.0402 mL	0.2008 mL	0.4017 mL	1.0042 mL
	60 mM	0.0335 mL	0.1674 mL	0.3347 mL	0.8368 mL
	80 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6276 mL
	100 mM	0.0201 mL	0.1004 mL	0.2008 mL	0.5021 mL

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Lu AF27139

P2X Receptor アイソフォーム固有の製品をすべて表示

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