Cat. No.: HY-160412

Balinatunfib

(Synonyms: SAR-441566; TNFα activity modulator 3)

Customer Review

Based on 1 Customer Validation

Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases.

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

Purity: 99.94%
CAS No.: 2248726-53-4
Formula: C₂₇H₂₄F₂N₆O₂
Molecular Weight:502.52

Storage:

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

Balinatunfib Chemical Structure

CAS No.: 2248726-53-4

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(In Japan)

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Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All TNF Receptor Isoforms :

In Vitro

Balinatunfib (1-1000 nM; 4 h) efficiently inhibits the expression of CD11b on granulocytes activated by Zymosan (HY-159069) in human whole blood, with an IC₅₀ of 35 nM and an IC₉₀ of 163 nM^[2].

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

In Vivo

Balinatunfib (1-30 mg/kg; oral administration; twice daily; 20 days) exerts improvement effects in a mouse arthritis model^[2].
Pharmacokinetic Analysis in Male Animals^[2]

Species	Route	Dose (mg/kg)	t_max (h)	C_max (ng/mL)	AUC_inf (ng.h/mL)	CL (L/h/kg)	V_z (L/kg)	T_1/2,z (h)	Bioavailability (%)
Rat	i.v.	1	/	424	731	1.38	4.1	2.1	/
Rat	p.o.	3	4	73.6	573	/	/	/	26
Dog	i.v.	1	/	1510	4200	0.267	2.68	7.00	/
Dog	p.o.	30	2	6920	131000	/	/	/	108
Dog	p.o.	100	7	6320	258000	/	/	/	62
Cynomolgus monkey	i.v.	1	/	774	2970	0.355	2.59	6.66	/
Cynomolgus monkey	p.o.	3	2	609	6620	/	/	/	67
Cynomolgus monkey	p.o.	10	6	1250	20000	/	/	/	68
Cynomolgus monkey	p.o.	20	8	2490	45200	/	/	/	77
Cynomolgus monkey	p.o.	100	6	3640	107000	/	/	/	36

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

Animal Model:

Male DBA/1 mice treated Collagen (HY-NP113)^[2]
Dosage:

1, 3, 10 and 30 mg/kg
Administration:

Oral administration; twice daily; 20 days
Result:

Showed a dose-dependent inhibition of arthritis symptoms. The 10 mg/kg dose group reduced the AUC of the disease score by 68%, and the 30 mg/kg dose group reduced it by 84%.
Protected the joint bone and improved bone microstructure parameters at doses of 10 mg/kg and 30 mg/kg.

Clinical Trial

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

Chemical Information

CAS No. 2248726-53-4
Appearance Solid
Molecular Weight 502.52
Formula C₂₇H₂₄F₂N₆O₂
Color White to off-white
SMILES

FC(F)OC1=C(C(C2=O)=CC=C1)[C@](C[C@@]3([H])N2C)([H])N4C3=NC5=CC=C(C6=CN=C(C7(CCC7)N)N=C6)C=C45
Synonyms

SAR-441566; TNFα activity modulator 3
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-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 (199.00 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

1.9900 mL

9.9499 mL

19.8997 mL

5 mM

0.3980 mL

1.9900 mL

3.9799 mL

10 mM

0.1990 mL

0.9950 mL

1.9900 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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: ≥ 5 mg/mL (9.95 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.95 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.95 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[1]. Nassr N, et al. First-in-Human Single and Multiple Ascending Dose Studies of Balinatunfib, a Small Molecule Inhibitor of TNFR1 Signaling in Healthy Participants. Clin Pharmacol Ther. 2025 Mar 30. [Content Brief]

[2]. Vugler A, et al. An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis. Front Pharmacol. 2022 Nov 16;13:1037983. doi: 10.3389/fphar.2022.1037983IF: 4.4 Q1 . Erratum in: Front Pharmacol. 2024 Oct 16;15:1479557. [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	1.9900 mL	9.9499 mL	19.8997 mL	49.7493 mL
	5 mM	0.3980 mL	1.9900 mL	3.9799 mL	9.9499 mL
	10 mM	0.1990 mL	0.9950 mL	1.9900 mL	4.9749 mL
	15 mM	0.1327 mL	0.6633 mL	1.3266 mL	3.3166 mL
	20 mM	0.0995 mL	0.4975 mL	0.9950 mL	2.4875 mL
	25 mM	0.0796 mL	0.3980 mL	0.7960 mL	1.9900 mL
	30 mM	0.0663 mL	0.3317 mL	0.6633 mL	1.6583 mL
	40 mM	0.0497 mL	0.2487 mL	0.4975 mL	1.2437 mL
	50 mM	0.0398 mL	0.1990 mL	0.3980 mL	0.9950 mL
	60 mM	0.0332 mL	0.1658 mL	0.3317 mL	0.8292 mL
	80 mM	0.0249 mL	0.1244 mL	0.2487 mL	0.6219 mL
	100 mM	0.0199 mL	0.0995 mL	0.1990 mL	0.4975 mL

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Balinatunfib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

All TNF Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Balinatunfib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

All TNF Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Balinatunfib Related Classifications

Cat. No.: HY-160412