製品番号: HY-103058

GSK199

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

GSK199 is an orally active, reversible, and selective PAD4 inhibitor with an IC₅₀ of 200 nM in the absence of calcium. GSK199 can be used for the research of rheumatoid arthritis.

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: 99.85%
CAS 番号: 1549811-53-1
分子式: C₂₄H₂₉ClN₆O₂
分子量:468.98

保管条件:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

GSK199 構造式

CAS 番号: 1549811-53-1

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生物活性

製品説明

GSK199 is an orally active, reversible, and selective PAD4 inhibitor with an IC₅₀ of 200 nM in the absence of calcium. GSK199 can be used for the research of rheumatoid arthritis^[1].

体外実験

GSK199 (0-20 μM, 72 h) inhibits viral genome production in a dose-dependent manner (IC₅₀ = 0.6 μM) in OC43-infected MRC-5 cells^[2].

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

体内実験

Pharmacokinetic Analysis in Male Balb/C Mice^[3]

Route	Dose (mg/kg)	AUC_0-∞ (ng·h/mL)	t_1/2 (h)	C_max (ng/mL)	F (%)
p.o.	10	4192	1.48	1.73	63.6
i.v.	2	1342	1.58	/	/

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

化学情報

CAS 番号 1549811-53-1
性状 Solid
分子量 468.98
分子式 C₂₄H₂₉ClN₆O₂
Color Light yellow to yellow
SMILES

O=C(N1C[C@H](N)CCC1)C2=CC(OC)=C3C(N=C(C4=CC5=CC=CN=C5N4CC)N3C)=C2.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (2)

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Int J Mol Sci

Targeting Peptidylarginine Deiminases in Neurons and Astrocytes in Central Nervous System Injury-Effects of Pan-PAD Inhibitor Cl-Amidine in an Oxygen-Glucose Deprivation Model of Ischaemia (OGD/R) and LPS Stimulation In Vitro. [Abstract]

2026 Jun 5;27(11):5118. PMID: 42278641
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (213.23 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

2.1323 mL

10.6614 mL

21.3229 mL

5 mM

0.4265 mL

2.1323 mL

4.2646 mL

10 mM

0.2132 mL

1.0661 mL

2.1323 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91. [Content Brief]

[2]. Pasquero S, et al. Novel antiviral activity of PAD inhibitors against human beta-coronaviruses HCoV-OC43 and SARS-CoV-2. Antiviral Res. 2022 Apr;200:105278. [Content Brief]

[3]. Hallur G, et al. LC-ESI-MS/MS Determination of GSK-199, A Novel Reversible PAD4 Inhibitor in Mice Plasma and its Application to a Pharmacokinetic Study in Mice. Pharm Anal Chem. 2017, 3(124): 40-1.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1323 mL	10.6614 mL	21.3229 mL	53.3072 mL
	5 mM	0.4265 mL	2.1323 mL	4.2646 mL	10.6614 mL
	10 mM	0.2132 mL	1.0661 mL	2.1323 mL	5.3307 mL
	15 mM	0.1422 mL	0.7108 mL	1.4215 mL	3.5538 mL
	20 mM	0.1066 mL	0.5331 mL	1.0661 mL	2.6654 mL
	25 mM	0.0853 mL	0.4265 mL	0.8529 mL	2.1323 mL
	30 mM	0.0711 mL	0.3554 mL	0.7108 mL	1.7769 mL
	40 mM	0.0533 mL	0.2665 mL	0.5331 mL	1.3327 mL
	50 mM	0.0426 mL	0.2132 mL	0.4265 mL	1.0661 mL
	60 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8885 mL
	80 mM	0.0267 mL	0.1333 mL	0.2665 mL	0.6663 mL
	100 mM	0.0213 mL	0.1066 mL	0.2132 mL	0.5331 mL

Keywords

GSK199

2 Cited Publications

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GSK199

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

MedChemExpress（MCE）の使用を引用している文献 GSK199

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GSK199

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

MedChemExpress（MCE）の使用を引用している文献 GSK199

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GSK199 関連分類

HY-103058 関連分類