Secukinumab
(Synonyms: 司库奇尤单抗; AIN457) 目录号 : GC19532
苏金单抗作为一种抗白细胞介素17A的单克隆抗体，通常用于治疗强直性脊柱炎。
Cas No.:875356-43-7
Sample solution is provided at 25 µL, 10mM.
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Secukinumab, as an anti-interleukin-17A monoclonal antibody, usually used for treatment with the ankylosing spondylitis[1].
In vitro experiment it indicated that when IL-17A at 956.2 ng/mL, secukinumab was obviously less potent[2].
In vivo clinical trail it suggested that treatment with 150 mg secukinumab subcutaneously or intravenously in patients remarkedly reduced the signs and symptoms of ankylosing spondylitis at week 16. While treatment with 75 mg secukinumab subcutaneously caused obvious improvement only with a higher intravenous loading dose.[1] Secukinumab has a highly favorable safety profile. In clinical test it demonstrated that treatment with 300 mg secukinumab, for occurs at a rate of 3.55/100 subject-years of mucocutaneous candidiasis, these infections usually do not interfere with maintenance of secukinumab therapy. Thus, secukinumab has an effictive new treatment for individuals with moderate-to-severe psoriasis.[3] In pivotal phase III trials, at dose of 75–150 mg and 75–300 mg secukinumab subcutaneously in pediatric patients aged 6 to < 18 years, there is an markedly improvemnet compared with placebo. It is suggested that secukinumab improved health-related quality of life and was generally well tolerated. [4] In efficacy trail it indicated that in received subcutaneous secukinumab 150?mg with (LD) or without (NL) loading dose patients or placebo weekly, secukinumab significantly improved the signs and symptoms of nr-axSpA across patients grouped by C-reactive protein (+/?) and/or magnetic resonance imaging (+/?) status, HLA-B27 (+/?) status, and sex[5].
References:
[1]Baeten D, et al. Secukinumab, an Interleukin-17A Inhibitor, in Ankylosing Spondylitis. N Engl J Med. 2015 Dec 24;373(26):2534-48.
[2]Adams R, et al. Bimekizumab, a Novel Humanized IgG1 Antibody That Neutralizes Both IL-17A and IL-17F. Front Immunol. 2020 Aug 21;11:1894.
[3]Blauvelt A. Safety of secukinumab in the treatment of psoriasis. Expert Opin Drug Saf. 2016 Oct;15(10):1413-20.
[4]Blair HA. Secukinumab: A Review in Moderate to Severe Pediatric Plaque Psoriasis. Paediatr Drugs. 2021 Nov;23(6):601-608.
[5]Braun J, et al. Secukinumab in non-radiographic axial spondyloarthritis: subgroup analysis based on key baseline characteristics from a randomized phase III study, PREVENT. Arthritis Res Ther. 2021 Sep 4;23(1):231.
苏金单抗作为一种抗白细胞介素17A的单克隆抗体,通常用于治疗强直性脊柱炎[1]。
体外实验表明,当IL-17A浓度为956.2 ng/mL时,苏金单抗的作用明显减弱[2]。
体内临床试验表明,在第 16 周时,皮下或静脉注射 150 mg 苏金单抗可显着减轻强直性脊柱炎的症状和体征。而皮下注射 75 mg 苏金单抗仅在较高的静脉负荷剂量下才会有明显改善.[1] 苏金单抗具有高度有利的安全性。在临床试验中,它证明用 300 mg 苏金单抗治疗,以 3.55/100 受试者年的比率发生皮肤粘膜念珠菌病,这些感染通常不会干扰苏金单抗治疗的维持。因此,苏金单抗对于中度至重度银屑病患者来说是一种有效的新疗法。[3]在关键的 III 期试验中,苏金单抗皮下注射 75-150 mg 和 75-300 mg 苏金单抗用于儿科6 岁至 < 的患者； 18年,与安慰剂相比有明显改善。这表明苏金单抗改善了与健康相关的生活质量,并且总体上耐受性良好。 [4] 在疗效试验中,它表明在每周接受皮下注射苏金单抗 150mg 负荷剂量 (LD) 或不负荷剂量 (NL) 或安慰剂的患者中,苏金单抗显着改善了 nr-axSpA 的体征和症状按 C 反应蛋白 (+/-) 和/或磁共振成像 (+/-) 状态、HLA-B27 (+/-) 状态和性别分组的患者[5]。
| Cell experiment [1]: | |
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Cell lines |
CMSC cells(Human chorionic derived mesenchymal stem cells) |
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Preparation Method |
Secukinumab was collected and purified from transduced CMSC cells. Cultured human dermal fibroblasts were incubated with IL-17A (15 ng/ml) in the presence of increasing concentrations of the secukinumab antibody(2-3 µg). After 48 hours the production of IL-6 in these cells was quantified using an ELISA kit (Abcam, UK) as an indicator of secukinumab functionality. |
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Reaction Conditions |
2-3 µg; 48h |
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Applications |
After 72 hours reduced IL-6 secretions from fibroblasts confirmed the inhibitory activity of secukinumab on human IL-17. |
| Animal experiment [2]: | |
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Animal models |
Balb/c female mice |
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Preparation Method |
The mice in the control group received 100 μL phosphate-buffered saline (PBS), while the mice in other groups received 100 μL (100 μg) BLM in PBS subcutaneously (sc) every day for 4 weeks. In addition, mice in groups 3 and 5 received secukinumab at a dose of 10 mg/kg/wk sc, and mice in the groups 4 and 5 received oral metformin 50 mg/kg/d for 28 days. |
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Dosage form |
10 mg/kg/wk sc |
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Applications |
Secukinumab and metformin ameliorated dermal fibrosis. |
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References: [1]. Fallah A, et al. Biosimilar Gene Therapy: Investigational Assessment of Secukinumab Gene Therapy. Cell J. 2020 Jan;21(4):433-443. [2]. Karatas A, et al. Secukinumab and metformin ameliorate dermal fibrosis by decreasing tissue interleukin-17 levels in bleomycin-induced dermal fibrosis. Int J Rheum Dis. 2021 Jun;24(6):795-802. |
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| Cas No. | 875356-43-7 | SDF | |
| 别名 | 司库奇尤单抗; AIN457 | ||
| 分子式 | C6584H10134N1754O2042S44 | 分子量 | 147941.89 |
| 溶解度 | 储存条件 | Store at 4°C, Do not freeze | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.0068 mL | 0.0338 mL | 0.0676 mL |
| 5 mM | 0.0014 mL | 0.0068 mL | 0.0135 mL |
| 10 mM | 0.0007 mL | 0.0034 mL | 0.0068 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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