Azaindole 1
(Synonyms: 6-氯-N4-[3,5-二氟-4-[(3-甲基-1H-吡咯并[2,3-B]吡啶-4-基)氧]苯基]-2,4-嘧啶二胺,ROCK-IN-2?，TC-S 7001) 目录号 : GC35442
A ROCK1 and ROCK2 inhibitor
Cas No.:867017-68-3
Sample solution is provided at 25 µL, 10mM.
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TC-S 7001 is an inhibitor of Rho-associated kinase (ROCK; IC50s = 0.6 and 1.1 nM, respectively, for human ROCK1 and ROCK2).1 It is selective for ROCK over myosin light-chain kinase (MLCK) and zipper-interacting protein kinase (ZIP-kinase; IC50s = 7,400 and 4,100 nM, respectively), as well as 110 kinases in a panel at 1-10 ?M, but does inhibit TRK and FLT3 (IC50s = 252 and 303 nM, respectively). TC-S 7001 reduces ROCK2-induced phosphorylation of human myosin-binding subunit (MBS) when used at a concentration of 3 nM and decreases ROCK2 autophosphorylation. It inhibits contraction of isolated rabbit saphenous artery induced by phenylephrine (IC50 = 65 nM) and decreases blood pressure in normotensive and hypertensive rats when administered at doses of 3 and 10 mg/kg. TC-S 7001 also decreases right ventricular systolic pressure and total pulmonary resistance in a rat model of monocrotaline-induced pulmonary hypertension when administered at a dose of 10 mg/kg per day.2
1.Kast, R., Schirok, H., Figueroa-Pérez, S., et al.Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinaseBr. J. Pharmacol.152(7)1070-1080(2007) 2.Dahal, B.K., Kosanovic, D., Pamarthi, P.K., et al.Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertensionEur. Respir. J.36(4)808-818(2010)
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Animal experiment: |
Male Wistar rats weighing 300-350 g are anaesthetized with thiopental 100 mg/kg intraperitoneally (i.p.). A tracheotomy is performed and catheters are inserted into the femoral artery for blood pressure and heart rate measurements and into the femoral vein for test drug administration. The animals are ventilated with room air and their body temperature is controlled. ROCK-IN-2 is administered intravenously (i.v.) in doses of 0.03-0.1 mg/kg. The vehicle Transcutol/Cremophor EL/physiological saline (19/10/80 = v/v/v) without test drug is used as control. The volume administered is 1 mL/kg. Six animals are treated per group[1]. |
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References: [1]. Kast R, et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. Epub 2007 Oct 15. |
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| Cas No. | 867017-68-3 | SDF | |
| 别名 | 6-氯-N4-[3,5-二氟-4-[(3-甲基-1H-吡咯并[2,3-B]吡啶-4-基)氧]苯基]-2,4-嘧啶二胺,ROCK-IN-2?，TC-S 7001 | ||
| Canonical SMILES | NC1=NC(Cl)=CC(NC2=CC(F)=C(OC3=C4C(NC=C4C)=NC=C3)C(F)=C2)=N1 | ||
| 分子式 | C18H13ClF2N6O | 分子量 | 402.79 |
| 溶解度 | DMSO: 33.33 mg/mL (82.75 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 2.4827 mL | 12.4134 mL | 24.8268 mL |
| 5 mM | 0.4965 mL | 2.4827 mL | 4.9654 mL |
| 10 mM | 0.2483 mL | 1.2413 mL | 2.4827 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