Ninerafaxstat (Synonyms: IMB-1018972; IMB-101)

Cat. No.: HY-139577 Purity: 90.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Ninerafaxstat (IMB-1018972) is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat can be used for research on cardiovascular diseases.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Ninerafaxstat trihydrochloride) usually boasts enhanced water solubility and stability.

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

Ninerafaxstat Chemical Structure

CAS No. : 2254741-41-6

Size	Price	Stock
5 mg	USD 370	Ask For Quote & Lead Time
10 mg	USD 590	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of Ninerafaxstat:

Ninerafaxstat trihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

3-KAT, fatty acid oxidation^[1].

In Vitro

Ninerafaxstat can reduce myocardial steatosis, improve left ventricular diastolic filling and myocardial energetics^[1].

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

In Vivo

Ninerafaxstat (30 mg/kg; once daily; 4 weeks; via osmotic minipump) can improve left ventricular systolic function and reduce left ventricular end diastolic pressure (LVEDP) and myocardial fibrosis in a mouse model of heart failure after myocardial infarction^[2].

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

Animal Model:	Murine model of post-MI HF^[2].
Dosage:	30 mg/kg
Administration:	Via osmotic minipump; once daily; 4 weeks
Result:	Increased left ventricular ejection fraction (LVEF) and reduced cardiac fibrosis.

Clinical Trial

Molecular Weight

415.48

Formula

C₂₂H₂₉N₃O₅

CAS No.

2254741-41-6

Appearance

Liquid (Density: 1.180±0.06 g/cm³)

Color

Colorless to light yellow

SMILES

O=C(C1=CC=CN=C1)OCCN2CCN(CC2)CC3=CC=C(C(OC)=C3OC)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (240.69 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	2.4069 mL	12.0343 mL	24.0685 mL
5 mM	0.4814 mL	2.4069 mL	4.8137 mL
10 mM	0.2407 mL	1.2034 mL	2.4069 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 (6.02 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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 (6.02 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (6.02 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

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: 90.94%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (245 KB) HNMR (137 KB) RP-HPLC (140 KB) LCMS (355 KB)

Handling Instructions (2659 KB)

References

[1]. Moritz Hundertmark MD, et al. Kiosk 11R-TC-08 - Ninerafaxstat Modulates Cardiac Energy Metabolism in Cardio-metabolic Syndromes: A Mechanistic, Hyperpolarized MR Trial. Journal of Cardiovascular Magnetic Resonance. 2024; 26: 100325.

[2]. Paul Chamberlin, et al. IMB-1018792, A NOVEL FIRST-IN CLASS PARTIAL FATTY ACID OXIDATION INHIBITOR IMPROVES CARDIAC REMODELING AND FUNCTION POST-MYOCARDIAL INFARCTION. J Am Coll Cardiol. 2021 May 11;77(18):539.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4069 mL	12.0343 mL	24.0685 mL	60.1714 mL
	5 mM	0.4814 mL	2.4069 mL	4.8137 mL	12.0343 mL
	10 mM	0.2407 mL	1.2034 mL	2.4069 mL	6.0171 mL
	15 mM	0.1605 mL	0.8023 mL	1.6046 mL	4.0114 mL
	20 mM	0.1203 mL	0.6017 mL	1.2034 mL	3.0086 mL
	25 mM	0.0963 mL	0.4814 mL	0.9627 mL	2.4069 mL
	30 mM	0.0802 mL	0.4011 mL	0.8023 mL	2.0057 mL
	40 mM	0.0602 mL	0.3009 mL	0.6017 mL	1.5043 mL
	50 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2034 mL
	60 mM	0.0401 mL	0.2006 mL	0.4011 mL	1.0029 mL
	80 mM	0.0301 mL	0.1504 mL	0.3009 mL	0.7521 mL
	100 mM	0.0241 mL	0.1203 mL	0.2407 mL	0.6017 mL

Ninerafaxstat Related Classifications

Metabolic Disease 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:

Ninerafaxstat2254741-41-6IMB-1018972 IMB-101IMB1018972IMB 1018972IMB101IMB 101IMB-101Mitochondrial Metabolismcardiac mitochondriafatty acidglucose oxidationcardiovascular diseaseInhibitorinhibitorinhibit

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