1,3-PBIT (dihydrobromide)
(Synonyms: 亚苯基-1,3-双(乙烷-2-异硫脲)二氢溴酸) 目录号 : GC11173
A potent inhibitor of iNOS
Cas No.:200716-66-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
1,3-PBIT (dihydrobromide) is a potent and selective iNOS inhibitor with Ki value of 47 nM [1].
Nitric oxide (NO) is an endogenously produced inorganic free radical gas which has been implicated in blood pressure homeostasis, platelet aggregation, neurotransmission, and immunological defense mechanisms. NO is synthesized by three isoforms of nitric oxide synthase (NOS): nNOS, eNOS and iNOS [1].
1,3-PBIT, also known as S,S’-(1,3-Phenylenebis(1,2-ethanediyl))bisisothiourea, is a potent and selective iNOS inhibitor. 1,3-PBIT inhibited purified human iNOS, eNOS and nNOS with Ki values of 47 nM, 9 μM and 0.25 μM, respectively. 1,3-PBIT exhibited 190-fold selective against iNOS versus eNOS. In DLD-1 cells, 1,3-PBIT inhibited human iNOS with IC50 value of 150 μM, presumably to poor membrane permeability [1].
In conscious male Sprague-Dawley rats, 1,3-PBIT (10mg/kg, ip; 1 h after endotoxin) inhibited endotoxin-induced decrease in MAP, renal CYP 4A1/A3 protein level and CYP 4A activity and increase in systemic and renal nitrite production [2].
References:
[1]. Garvey EP, Oplinger JA, Tanoury GJ, et al. Potent and selective inhibition of human nitric oxide synthases. Inhibition by non-amino acid isothioureas. J Biol Chem. 1994 Oct 28;269(43):26669-76.
[2]. Tunctan B, Yaghini FA, Estes A, et al. Inhibition by nitric oxide of cytochrome P450 4A activity contributes to endotoxin-induced hypotension in rats. Nitric Oxide. 2006 Feb;14(1):51-7.
| Cas No. | 200716-66-1 | SDF | |
| 别名 | 亚苯基-1,3-双(乙烷-2-异硫脲)二氢溴酸 | ||
| 化学名 | S,S'-1,3-phenylene-bis(1,2-ethanediyl)bis-isothiourea, dihydrobromide | ||
| Canonical SMILES | N/C(SCCC1=CC(CCS/C(N)=N/[H])=CC=C1)=N/[H].Br.Br | ||
| 分子式 | C12H18N4S2 • 2HBr | 分子量 | 444.2 |
| 溶解度 | ≤100mg/ml in Water | 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 | 2.2512 mL | 11.2562 mL | 22.5124 mL |
| 5 mM | 0.4502 mL | 2.2512 mL | 4.5025 mL |
| 10 mM | 0.2251 mL | 1.1256 mL | 2.2512 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。