Sitaxentan sodium
(Synonyms: 西他生坦钠,IPI 1040 sodium; TBC11251 sodium) 目录号 : GC17769
Sitaxentan sodium是一种选择性内皮素A受体（ETA）拮抗剂（IC50 = 1.4nM；Ki = 0.43nM）。
Cas No.:210421-74-2
Sample solution is provided at 25 µL, 10mM.
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Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist (IC50 = 1.4 nM; Ki = 0.43nM) [1]. Sitaxentan sodium selectively blocks the action of endothelin (ET) on endothelin A (ETA) receptors [2]. Sitaxentan sodium is often used to treat pulmonary hypertension [3].
In Surgery for wire injury mouse model, Sitaxentan sodium (15mg/kg; po; 28d) inhibits the formation of neointimal lesions in femoral arteries of mice [4]. In rat toxicity experiments, Sitaxentan sodium (10, 30, 60mg/kg; po; 9 weeks) did not affect the survival, clinical symptoms, or body weight of rats [5]. In humanized liver chimeric mice, triglyceride (TG) levels in mice treated with Sitaxentan sodium (10mg/kg; po; single dose) were significantly increased [6].
References:
[1]. Tilton RG, Munsch CL, Sherwood SJ, et al. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ETAreceptor antagonist. Pulmonary pharmacology & therapeutics. 2000 Apr 1; 13(2): 87-97.
[2]. Rondelet B, Dewachter L, Kerbaul F, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension. American Journal of Physiology-Heart and Circulatory Physiology. 2010 Oct;299(4):H1118-H1123.
[3]. Barst RJ, Langleben D, Frost A, et al. Sitaxsentan therapy for pulmonary arterial hypertension. American journal of respiratory and critical care medicine. 2004 Feb 15;169(4):441-447.
[4]. Duthie KM, Hadoke PW, Kirkby NS, et al. Selective endothelin A receptor antagonism with sitaxentan reduces neointimal lesion size in a mouse model of intraluminal injury. British Journal of Pharmacology. 2015 Jun; 172(11): 2827-2837.
[5]. Cross DM, Derzi M, Horsley E, et al. Evaluation of sitaxentan (Thelin®) toxicity in juvenile rats and regulatory interactions during the development of a European Medicines Agency pediatric investigation plan. Regulatory Toxicology and Pharmacology. 2012 Oct 1; 64(1): 43-50.
[6]. King A, Baginski M, Morikawa Y, et al. Application of a novel mass spectral data acquisition approach to lipidomic analysis of liver extracts from sitaxentan-treated liver-humanized PXB mice. Journal of proteome research. 2019 Sep 24; 18(11): 4055-4064.
Sitaxentan sodium是一种选择性内皮素A受体（ETA）拮抗剂（IC50 = 1.4nM；Ki = 0.43nM）[1]。Sitaxentan sodium选择性阻断内皮素（ET）对内皮素A受体（ETA）的作用 [2]。Sitaxentan sodium常用于治疗肺动脉高压 [3]。
在钢丝损伤手术小鼠模型中，Sitaxentan sodium（15mg/kg；po；28d）可抑制小鼠股动脉新生内膜病变的形成 [4]。在大鼠毒性实验中，Sitaxentan sodium（10、30、60mg/kg；po；9周）对大鼠的生存期、临床症状和体重均无影响 [5]。在人源化肝嵌合小鼠中，用Sitaxentan sodium（10mg/kg；po；单剂量）治疗的小鼠的甘油三酯（TG）水平显著升高 [6]。
| Animal experiment [1]: | |
Animal models | Surgery for wire injury mouse model |
Preparation Method | The orally active selective ETA receptor antagonist Sitaxentan sodium (15mg/kg), were administered by admixture with chow. Each compound was prepared by dispersion in 0.2% methylcellulose and bound with RM1 mouse chow using beef gelatine and fresh diet was provided daily. Drug administration was started 1 week before surgery for wire injury and continued for a further 28 days. |
Dosage form | 15mg/kg; po; 28d |
Applications | Sitaxentan sodium inhibits the formation of neointimal lesions in femoral arteries of mice. |
References: | |
| Cas No. | 210421-74-2 | SDF | |
| 别名 | 西他生坦钠,IPI 1040 sodium; TBC11251 sodium | ||
| 化学名 | sodium;(4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide | ||
| Canonical SMILES | CC1=CC2=C(C=C1CC(=O)C3=C(C=CS3)S(=O)(=O)[N-]C4=C(C(=NO4)C)Cl)OCO2.[Na+] | ||
| 分子式 | C18H14ClN2NaO6S2 | 分子量 | 476.89 |
| 溶解度 | ≥ 23.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.0969 mL | 10.4846 mL | 20.9692 mL |
| 5 mM | 0.4194 mL | 2.0969 mL | 4.1938 mL |
| 10 mM | 0.2097 mL | 1.0485 mL | 2.0969 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。
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet