SC 560
(Synonyms: 5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑) 目录号 : GC15634
A selective inhibitor of COX-1
Cas No.:188817-13-2
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.009 μM for COX-1; 6.3 μM for COX-2
SC-560 [5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-trif luoromethylpyrazole] is a COX-1-selective inhibitor, which can be used as a pharmacological tool to study the role of COX-1-derived PGs in inflammation and pain. COX-1 is an enzyme that is responsible for formation of prostanoids, including thromboxane and prostaglandins.
In vitro: Preincubation of COX-1 with SC-560 inhibited the conversion of arachidonic acid to PGE2 in a concentration-dependent manner [1]. SC-560 was necessary to sustain a reduced basal level of PGI2 for an extended period. SC-560 inhibits cell proliferation and accelerates apoptosis which results in attenuated tumor growth [2].
In vivo: Oral dosing with either 10 or 30 mg/kg SC-560 1 hr before assay completely inhibited COX-1-derived platelet thromboxane B2, gastric PGE2, and dermal PGE2 production [1]. SC-560 can suppress ovarian surface epithelial tumor growth. Tumor growth was suppressed in allografted mice treated with SC-560 for a longer period, but the reduction in tumor growth was less dramatic than the short-term treated [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Daikoku T, Wang D, Tranguch S, Morrow JD, Orsulic S, DuBois RN, Dey SK. Cyclooxygenase-1 is a potential target for prevention and treatment of ovarian epithelial cancer. Cancer Res. 2005 May 1;65(9):3735-44.
[2] Christopher J. Smith, Yan Zhang, Carol M. Koboldt, Jerry Muhammad, Ben S. Zweifel, Alex Shaffer, John J. Talley, Jaime L. Masferrer, Karen Seibert, Peter C. Isakson. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci U S A. 1998 Oct 27; 95(22): 13313–13318.
Cell experiment: | HuH-6 and HA22T/VGH cells (5000/well) are treated with various concentrations of SC-560 (5, 10, 25, 50, 100, 200 μM) and cultured for 72 h. At the end of treatment, cell viability is assessed by MTS assay[2]. |
Animal experiment: | Rats: The pharmacokinetics of SC-560 is studied in Sprague-Dawley rats after a single intravenous (i.v.) and oral dose (10 mg/kg) in polyethylene glycol (PEG) 600 and a single oral dose (10 mg/kg) in 1% methylcellulose (MC). Serial blood samples are collected via a catheter inserted in the right jugular vein and serum samples are analysed for SC-560 using reverse phase HPLC. After oral administration of SC-560 in PEG, urine is also collected for 24 h and analyzed for urinary sodium, chloride, and potassium as well as NAG[3]. |
References: [1]. Smith CJ, et al. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13313-8. | |
| Cas No. | 188817-13-2 | SDF | |
| 别名 | 5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑 | ||
| 化学名 | 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole | ||
| Canonical SMILES | ClC1=CC=C(C=C1)C2=CC(C(F)(F)F)=NN2C(C=C3)=CC=C3OC | ||
| 分子式 | C17H12ClF3N2O | 分子量 | 352.74 |
| 溶解度 | ≥ 35.3mg/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 | 2.8349 mL | 14.1747 mL | 28.3495 mL |
| 5 mM | 0.567 mL | 2.8349 mL | 5.6699 mL |
| 10 mM | 0.2835 mL | 1.4175 mL | 2.8349 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet