製品番号: HY-156438

Ruvonoflast

(別名: NT-0796)

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Based on 1 Customer Validation

Ruvonoflast (NT-0796) is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. Ruvonoflast inhibits IL-1β release in human PBMC cells with an IC₅₀ value of 0.32 nM. Ruvonoflast is an isopropyl ester that undergoes intracellular conversion to Ruvonoflast, the carboxylic acid active species. Ruvonoflast reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. Ruvonoflast is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis.

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純度: 99.29%
CAS 番号: 2272917-13-0
分子式: C₂₃H₂₇N₃O₄
分子量:409.48

保管条件:

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

Ruvonoflast 構造式

CAS 番号: 2272917-13-0

容量

価格（税別）

在庫状況

数量

Sample (0.1mg)

In-stock

(In Japan)

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

生物活性

製品説明

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示 :

Interleukin Related 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
PBMC	IC₅₀	>2 μM Compound: NT-0796	Inhibition of LPS-induced IL-6 secretion in human PBMC cells incubated for 4 hrs by ELISA Inhibition of LPS-induced IL-6 secretion in human PBMC cells incubated for 4 hrs by ELISA	[PMID: 37874905]
PBMC	IC₅₀	>2 μM Compound: NT-0796	Inhibition of LPS-induced TNFalpha secretion in human PBMC cells incubated for 4 hrs by ELISA Inhibition of LPS-induced TNFalpha secretion in human PBMC cells incubated for 4 hrs by ELISA	[PMID: 37874905]

体外実験

Ruvonoflast (NT-0796) (0.0001-10 μM, 60 min) inhibits IL-1β output from human peripheral blood mononuclear cells (PBMCs) stimulated with LPS (HY-D1056) and ATP, also inhibits IL-1β output in the context of human blood yielding IC₅₀ values of 3.4 μM and 0.009 μM, respectively^[3].

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

体内実験

Ruvonoflast (NT-0796) (3 mg/kg, i.v., a single dose for 5 min) is CNS penetrant and undergoes intracellular conversion to NDT-19795 (the carboxylic acid active species) in mice^[1].
Ruvonoflast (3- 100 mg/kg, p.o., three times a day for 15 weeks) leads to a significant weight loss and reduces circulating levels of fibrinogen, sVCAM-1, suPAR and plasma LDL levels in diet-induced obesity (DIO) mice^[3].

Blood and Brain Concentrations of NT-0796 after 5 min Following iv Administration of Ruvonoflast at 3 mg/kg in C57BL/6 Mice^[1]

	blood concentration (ng/mL)	brain concentration (ng/g)	brain/blood ratio
NT-0796	610	479	0.79

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

Animal Model:

Mice^[1]
Dosage:

3 mg/kg
Administration:

i.v., a single dose for 5 min
Result:

Was shown to be CNS penetrant, with a brain-to-blood ratio of 0.79 in mice.

Animal Model:

Diet-induced obesity mice^[3]
Dosage:

3- 100 mg/kg
Administration:

p.o., three times a day for 15 weeks
Result:

Reduced body fat in DIO mice by 31.8% over 28 days.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2272917-13-0
性状 Solid
分子量 409.48
分子式 C₂₃H₂₇N₃O₄
Color White to off-white
SMILES

CC(C)OC([C@H](OC(NC1=C2C(CCC2)=CC3=C1CCC3)=O)CC4=NC=CC=N4)=O
別名

NT-0796
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 : 100 mg/mL (244.21 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

2.4421 mL

12.2106 mL

24.4212 mL

5 mM

0.4884 mL

2.4421 mL

4.8842 mL

10 mM

0.2442 mL

1.2211 mL

2.4421 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

濃度

体積

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)

体積 _(開始)

濃度 _(終了)

体積 _(終了)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
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.

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 (277 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[1]. David Harrison, et al. Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders. J Med Chem. 2023 Oct 24. [Content Brief]

[2]. Thornton P, et al. Reversal of High Fat Diet-Induced Obesity, Systemic Inflammation, and Astrogliosis by the NLRP3 Inflammasome Inhibitors NT-0249 and NT-0796. J Pharmacol Exp Ther. 2024 Feb 15;388(3):813-826. [Content Brief]

[3]. Smolak P, et al. Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency. J Pharmacol Exp Ther. 2024 Feb 15;388(3):798-812. [Content Brief]

[4]. Doedens JR, et al. The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1. Biochem Pharmacol. 2024 Sep;227:116455. [Content Brief]

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	2.4421 mL	12.2106 mL	24.4212 mL	61.0530 mL
	5 mM	0.4884 mL	2.4421 mL	4.8842 mL	12.2106 mL
	10 mM	0.2442 mL	1.2211 mL	2.4421 mL	6.1053 mL
	15 mM	0.1628 mL	0.8140 mL	1.6281 mL	4.0702 mL
	20 mM	0.1221 mL	0.6105 mL	1.2211 mL	3.0527 mL
	25 mM	0.0977 mL	0.4884 mL	0.9768 mL	2.4421 mL
	30 mM	0.0814 mL	0.4070 mL	0.8140 mL	2.0351 mL
	40 mM	0.0611 mL	0.3053 mL	0.6105 mL	1.5263 mL
	50 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2211 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0176 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7632 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6105 mL

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Ruvonoflast

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Inflammasomes related Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示

Interleukin Related アイソフォーム固有の製品をすべて表示

生物活性

化学情報

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

Ruvonoflast

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Inflammasomes related Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示

Interleukin Related アイソフォーム固有の製品をすべて表示

生物活性

化学情報

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

Ruvonoflast 関連分類

製品番号: HY-156438