Nexinhib20

Cat. No.: HY-125792 Purity: 99.69%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Nexinhib20 is an inhibitor that targets the interactions of Rab27a-JFC1 (IC₅₀: 2.6 μM) and Rac-1-GTP. Nexinhib20 can inhibit neutrophil exocytosis, adhesion, and β2 integrin activation, and has anti-inflammatory activity. Nexinhib20 can be used in the research of diseases such as systemic inflammation and myocardial ischemia-reperfusion injury.

For research use only. We do not sell to patients.

Nexinhib20 Chemical Structure

CAS No. : 331949-35-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 2.6 μM (Rab27a-JFC1 interaction)^[1]

In Vitro

Nexinhib20 (10 μM; 1 h) can inhibit the secretion of myeloperoxidase, the production of superoxide anions, and also inhibit the upregulation of adhesion molecules and receptors, such as CD11b and CD66b in neutrophils^[1].
Nexinhib20 (10 μM; 1 h) can inhibit the IL-8-induced adhesion of human neutrophils to P-selectin and ICAM-1, the exocytosis and activation of β2 integrin, as well as the intracellular calcium flux and the activation of Rac-1^[2].

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

In Vivo

Nexinhib20 (100 mM; 10 μL; intraperitoneal injection; single dose) has a protective effect in a mouse model of myocardial I/R injury^[2].

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

Animal Model:	C57BL/6J mice with ischemia-reperfusion injury^[2]
Dosage:	100 mM; 10 μL
Administration:	Intraperitoneal injection (i.p.); single dose
Result:	Significantly decreased infarct size (white area in the TTC-phthalo-blue-staining) after myocardial I/R injury. Limited neutrophil recruitment to the coronary artery. Improved left ventricular function.

Molecular Weight

300.31

Formula

C₁₅H₁₆N₄O₃

CAS No.

331949-35-0

Appearance

Solid

Color

White to yellow

SMILES

O=C(/C(N1N=CN=C1)=C/C2=CC=CC([N+]([O-])=O)=C2)C(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (332.99 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	3.3299 mL	16.6495 mL	33.2989 mL
5 mM	0.6660 mL	3.3299 mL	6.6598 mL
10 mM	0.3330 mL	1.6649 mL	3.3299 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (8.32 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.32 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/1% Tween-80 in Saline water
Solubility: 5.05 mg/mL (16.82 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.69%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (249 KB) HNMR (278 KB) RP-HPLC (243 KB) LCMS (116 KB)

Handling Instructions (2659 KB)

References

[1]. Johnson JL, et al. Identification of Neutrophil Exocytosis Inhibitors (Nexinhibs), Small Molecule Inhibitors of Neutrophil Exocytosis and Inflammation: DRUGGABILITY OF THE SMALL GTPase Rab27a. J Biol Chem. 2016 Dec 9;291(50):25965-25982. [Content Brief]

[2]. Liu W, et al. Nexinhib20 Inhibits Neutrophil Adhesion and β2 Integrin Activation by Antagonizing Rac-1-Guanosine 5'-Triphosphate Interaction. J Immunol. 2022 Oct 15;209(8):1574-1585. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3299 mL	16.6495 mL	33.2989 mL	83.2473 mL
	5 mM	0.6660 mL	3.3299 mL	6.6598 mL	16.6495 mL
	10 mM	0.3330 mL	1.6649 mL	3.3299 mL	8.3247 mL
	15 mM	0.2220 mL	1.1100 mL	2.2199 mL	5.5498 mL
	20 mM	0.1665 mL	0.8325 mL	1.6649 mL	4.1624 mL
	25 mM	0.1332 mL	0.6660 mL	1.3320 mL	3.3299 mL
	30 mM	0.1110 mL	0.5550 mL	1.1100 mL	2.7749 mL
	40 mM	0.0832 mL	0.4162 mL	0.8325 mL	2.0812 mL
	50 mM	0.0666 mL	0.3330 mL	0.6660 mL	1.6649 mL
	60 mM	0.0555 mL	0.2775 mL	0.5550 mL	1.3875 mL
	80 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0406 mL
	100 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8325 mL

Nexinhib20 Related Classifications

Inflammation/Immunology Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
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.

Keywords:

Nexinhib20331949-35-0Nexinhib 20Nexinhib-20Reactive Oxygen SpeciesRasIntegrinischemia-reperfusion injury modelneutrophilsInhibitorinhibitorinhibit

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