GLPBio

Balinatunfib (SAR-441566)

Catalog No.: GC73867Purity:>98.00%
COASDSData Sheet
TNFα activity modulator 3의 (6) 예는 변조기 TNF 활동을 억제 TNF α-induced NF-κ B 활성화 및 관련 연구에서 사용 될 수 있다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.

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
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

인용 문헌 (Citations)

현재 이 제품에 대한 인용 문헌이 없습니다. 아래는 GlpBio 제품을 인용한 주요 논문입니다.
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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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    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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    388(6745) (2025)
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    387(6734) (2025)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

제품 설명 (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.

실험 프로토콜 (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.

제품 문서 (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

화학적 특성 (Chemical Properties)

CAS 번호
2248726-53-4
분자식
C27H24F2N6O2
분자량
502.52
용해도
DMSO : 116.67 mg/mL (232.17 mM; Need ultrasonic)
보관
-20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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