ATB-343
目录号 : GC16245
A H2S-releasing NSAID
Cas No.:1000700-26-4
Sample solution is provided at 25 µL, 10mM.
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ATB-343, also named as indomethacin, is an H2S-releasing derivative of indomethacin [1].
Hydrogen sulfide (H2S) is a newly recognized signaling molecule with potent cytoprotective actions. Hydrogen sulfide has been involved in mediating many physiological processes, such as the maintenance of gastrointestinal mucosal defense and repair. Hydrogen sulfide also exerts many anti-inflammatory effects, including inhibition of leukocyte adherence to the vascular endothelium and leukocyte migration to sites of inflammation [2].
In vitro: Indomethacin enhanced the NK cell activity in vitro by blocking the prostaglandin production of monocytes [3].
In vivo: In rats, oral administration of ATB-343 significantly inhibited gastric prostaglandin synthesis and systemic COX-1 activity [1]. Indomethacin was a potent inhibitor of prostaglandin synthesis. Indomethacin suppressed in vivo thyroid hormone secretion and cholera toxin-induced intestinal fluid accumulation. Indomethacin in submicromolar concentrations inhibited cyclic AMP-dependent protein kinase and endogenous protein phosphorylation [4].
Clinical trials: Indomethacin has entered clinical trial in Alzheimer's disease [5].
References:
[1] Wallace J L. Hydrogen sulfide-releasing anti-inflammatory drugs[J]. Trends in Pharmacological Sciences, 2007, 28(10): 501-505.
[2] Wallace J L. Physiological and pathophysiological roles of hydrogen sulfide in the gastrointestinal tract[J]. Antioxidants & redox signaling, 2010, 12(9): 1125-1133.
[3] Pedersen B K, Oxholm P, Klarlund K. Characterization of the in vivo and in vitro effects of indomethacin on human natural killer cell activity[J]. Allergy, 1986, 41(7): 532-536.
[4] Kantor H S, Hampton M. Indomethacin in submicromolar concentrations inhibits cyclic AMP-dependent protein kinase[J]. 1978.
[5] Rogers J, Kirby L C, Hempelman S R, et al. Clinical trial of indomethacin in Alzheimer's disease[J]. Neurology, 1993, 43(8): 1609-1609.
| Cas No. | 1000700-26-4 | SDF | |
| 化学名 | 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-4-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl ester-1H-indole-3-acetic acid | ||
| Canonical SMILES | COc1ccc2c(c1)c(CC(=O)Oc1ccc(cc1)c1ssc(=S)c1)c(C)n2C(=O)c1ccc(Cl)cc1 | ||
| 分子式 | C28H20ClNO4S3 | 分子量 | 566.1 |
| 溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 1.7665 mL | 8.8324 mL | 17.6647 mL |
| 5 mM | 0.3533 mL | 1.7665 mL | 3.5329 mL |
| 10 mM | 0.1766 mL | 0.8832 mL | 1.7665 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet