GLPBio

Balinatunfib (SAR-441566)

Catalog No.: GC73867Purity:>98.00%
COASDSData Sheet
TNFα activity modulator 3 (exemple 6) est un modulateur de l’activité du TNF qui inhibe l’activation du NF-κB induit par le tnfα et peut être utilisé dans des recherches pertinentes.

Les produits sont exclusivement destinés à la recherche. Ils ne doivent pas être utilisés chez l’être humain. Nous ne vendons pas aux patients.

Balinatunfib (SAR-441566)
Cas No.: 2248726-53-4
10mM (in 1mL DMSO)In Stock
$226.00
1
1mgIn Stock
$102.00
1
5mgIn Stock
$205.00
1
10mgIn Stock
$287.00
1
25mgIn Stock
$477.00
1
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Citations

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    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Description

Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling [1]. Balinatunfib can change the configuration of the soluble TNFα (sTNFα) trimer and prevents the heterotrimerization with TNFR1 but not TNFR2, thereby blocking TNFR1 signaling [2]. Balinatunfib has been widely used to inhibit the production of pro-inflammatory cytokines and to alleviate psoriasis [3].

In vitro, Balinatunfib treatment for 1 hour significantly inhibited zymosan-activated CD11b expression on granulocytes in human whole blood, with an IC50 value of 35nM[4].

In vivo, Balinatunfib treatment via oral administration at a dose of 30mg/kg twice daily for 20 days, significantly inhibited the development of arthritis in DBA/1 mice and promoted the improvement of bones[4].

References:
[1] Drakos A, Torres T, Vender R. Emerging oral therapies for the treatment of psoriasis: a review of pipeline agents[J]. Pharmaceutics, 2024, 16(1): 111.
[2] Nassr N, Rharbaoui F, Weitz D, et al. First‐in‐Human Single and Multiple Ascending Dose Studies of Balinatunfib, a Small Molecule Inhibitor of TNFR1 Signaling in Healthy Participants[J]. Clinical Pharmacology & Therapeutics, 2025, 118(1): 164-176.
[3] Leung A, Marquez-Grap G, Kranyak A, et al. A review of spatial transcriptomics in psoriasis: new insights into cellular contributions[J]. Current Opinion in Immunology, 2025, 95: 102585.
[4] Vugler A, O’Connell J, Nguyen M A, et al. An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis[J]. Frontiers in pharmacology, 2022, 13: 1037983.

Protocole (Protocol)

Animal experiment [1]:

Animal models

Male DBA/1 mice

Preparation Method

Male DBA/1 mice were maintained in a controlled environment at 22±3°C and 60% relative humidity under a 12h light/dark cycle, and were given free access to standard rodent nutrition and water. Chicken type II collagen (CII) was dissolved in 0.1M acetic acid at a concentration of 2mg/ml and rolled overnight at 4°C. The next day (Day 0) the CII solution was emulsified in an equal volume of complete Freund’s adjuvant to give a final concentration of 1mg/ml. Mice aged 10-15 weeks old were sensitized with 0.1ml (100µg CII) of emulsion injected intradermally on the flank under anesthesia. Fourteen days post-sensitization mice received a booster intradermal injection of CII emulsified in incomplete Freund’s adjuvant on the opposite flank. Mice were assessed for signs of arthritis from Day 14 onwards. When signs of arthritis were seen, mice were weighed, and disease scored. The disease score was graded on a 0 to 3 scale as follows: grade 0, no swelling; grade 1, wrist or ankle swollen; grade 2, wrist/ankle and pad swollen; grade 3, wrist/ankle, pad, and digits swollen. The disease score was the sum of all 4 paws (the maximum score per mouse was 12). Mice were dosed therapeutically for 20 days with either vehicle or Balinatunfib (orally twice a day) starting from the first day they showed signs of arthritis. The efficacy of SAR441566 was assessed at a dose of 30mg/kg.

Dosage form

30mg/kg; twice a day for 20 days; p.o.

Applications

Balinatunfib treatment inhibited arthritis development in collagen-induced arthritis mice.

References:
[1] Vugler A, O’Connell J, Nguyen M A, et al. An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis[J]. Frontiers in pharmacology, 2022, 13: 1037983.

Documents produit (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propriétés chimiques (Chemical Properties)

N° CAS
2248726-53-4
Formule moléculaire
C27H24F2N6O2
Masse moléculaire
502.52
Solubilité
DMSO : 116.67 mg/mL (232.17 mM; Need ultrasonic)
Conservation
-20°C
Conseils généraux
Choisissez un solvant adapté selon les données de solubilité du produit. Après préparation, répartissez la solution mère en aliquotes afin d’éviter les cycles répétés de congélation-décongélation.
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Conditions d’expédition
Les échantillons d’évaluation sont expédiés avec des blocs réfrigérants. Les autres formats sont expédiés à température ambiante ou, sur demande, avec des blocs réfrigérants.

Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité

g/mol

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