Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

H-151 [941987-60-6]

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Katalog-Nummer NB-64-30079-50mg

Size : 50mg

Marke : Neo Biotech

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H-151

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Synonyms:

Catalog No. T5674 Copy Product Info

Purity: 99.97%

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H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

Cas No. 941987-60-6

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.97%

Appearance:Solid

Color:White

Product Introduction

Bioactivity

Description	H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.
Targets & IC50	BMDMs:109.6 nM, HFF cells:134.4 nM, MEF cells:138 nM
In vitro	METHODS: Mouse monocyte macrophage RAW264.7 was treated with H-151 (0.25-2 μM) for 1 h, and then stimulated with rmCIRP (1 μg/mL) for 24 h. The level of IFN-β was measured by ELISA. RESULTS: IFN-β was dose-dependently reduced in the culture supernatant of cells pretreated with H-151, which inhibited eCIRP-induced activation of STING in vitro. [1] METHODS: Human monocytes THP-1 were treated with H-151 (0.5 μM) for 2 h, and the expression levels of target proteins were measured by Western Blot. RESULTS: H-151 inhibited the phosphorylation of TBK1, and H-151 effectively inhibited the activation of hsSTING. [2]
In vivo	METHODS: To assay in vivo activity, H-151 (750 nmol, 200 μL) was administered intraperitoneally to Trex1-/- Ifnb1Δβ-luc/Δβ-luc reporter mice once daily for seven days. RESULTS: When administered for one week, H-151 showed significant efficacy in Trex1-/- mice expressing a bioluminescent IFNβ reporter gene. [2] METHODS: To test the role in cisplatin-induced acute kidney injury (AKI), H-151 (7 mg/kg) was administered intraperitoneally to C57BL/6J mice with cisplatin-induced AKI three times a day. RESULTS: H-151 treatment significantly ameliorated cisplatin-induced renal injury, as evidenced by improvement in renal function, renal morphology, and renal inflammation.H-151 may be a potential therapeutic agent for the treatment of AKI, possibly by inhibiting STING-mediated inflammation and mitochondrial damage. [3]

Chemical Properties

Molecular Weight	279.34
Formula	C₁₇H₁₇N₃O
Cas No.	941987-60-6
Smiles	CCc1ccc(NC(=O)Nc2c[nH]c3ccccc23)cc1
Relative Density.	1.298 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 14.08 mg/mL (50.4 mM), Sonication is recommended.

DMSO: 100 mg/mL (357.99 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 12.5 mg/mL (44.75 mM), Suspension.

5% DMSO+40% PEG300+5% Tween 80+50% Saline: 5 mg/mL (17.9 mM)

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5799 mL	17.8993 mL	35.7987 mL	178.9933 mL
5 mM	0.7160 mL	3.5799 mL	7.1597 mL	35.7987 mL
10 mM	0.3580 mL	1.7899 mL	3.5799 mL	17.8993 mL
20 mM	0.1790 mL	0.8950 mL	1.7899 mL	8.9497 mL
50 mM	0.0716 mL	0.3580 mL	0.7160 mL	3.5799 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0358 mL	0.1790 mL	0.3580 mL	1.7899 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Keywords

TMEM173TBK1STINGStimulator of Interferon GenesphosphorylationpalmitoylatioMPYSMITAInhibitorinhibitH-151H151H 151ERISautoinflammatory

Related Tags: H-151 chemical structure | H-151 in vivo | H-151 in vitro | H-151 formula | H-151 molecular weight