GLPBio

Balinatunfib (SAR-441566)

Catalog No.: GC73867Purity:>98.00%
COASDSData Sheet
Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling.

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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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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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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.

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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
2248726-53-4
Molecular Formula
C27H24F2N6O2
Molecular Weight
502.52
Solubility
DMSO : 116.67 mg/mL (232.17 mM; Need ultrasonic)
Storage
-20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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