GLPBio

Balinatunfib (SAR-441566)

Catalog No.: GC73867Purity:>98.00%
COASDSData Sheet
TNFα activity modulator 3(例6)は変調器TNF活動TNFを抑えるα-induced NF -κB・活性化や関連研究に利用することができる。

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。

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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引用文献 (Citations)

現在、この製品の引用文献はありません。以下はGlpBio製品を引用した代表的な文献です。
  • Nature cover
    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)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    Science
    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    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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    Cell Research
    31, 1291–1307 (2021)

製品説明 (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.

実験プロトコル (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.

製品資料 (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

化学的性質 (Chemical Properties)

CAS番号
2248726-53-4
分子式
C27H24F2N6O2
分子量
502.52
溶解性
DMSO : 116.67 mg/mL (232.17 mM; Need ultrasonic)
保存条件
-20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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