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Y-27632 dihydrochloride

Y-27632 dihydrochloride

产品编号 T1725   CAS 129830-38-2
别名: 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐, Y-27632 2HCl

Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂,具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡

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Y-27632 dihydrochloride Chemical Structure
Y-27632 dihydrochloride, CAS 129830-38-2
规格 价格/CNY 货期 数量
1 mg ¥ 248 现货
2 mg ¥ 352 现货
5 mg ¥ 578 现货
10 mg ¥ 745 现货
25 mg ¥ 1,450 现货
50 mg ¥ 2,650 现货
100 mg ¥ 3,290 现货
200 mg ¥ 4,790 现货
500 mg ¥ 7,570 现货
1 mL * 10 mM (in DMSO) ¥ 637 现货
其他形式的 Y-27632 dihydrochloride:
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Y-27632 dihydrochloride (T1725)
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参考文献
产品描述 Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
靶点活性 ROCK1 (p160ROCK):140 nM (Ki, cell free), ROCK2:300 nM (Ki, cell free)
体外活性 方法:人诱导多能干细胞 marmoset iPSC 用 Y-27632 (5-20 μM) 处理 7 天,使用 AKP 检测克隆形成情况。
结果:Y-27632 显著提高 marmoset iPSC 的克隆效率。[1]
方法:成人脂肪组织衍生干细胞 ADSCs 用 Y-27632 (5 μmol/L) 处理 1 h,检测 ADSCs 的形态变化。
结果:Y-27632 剂量依赖性诱导 ADSCs 的神经元分化,5 μmol/L Y-27632 处理 1 h 的 ADSCs的神经元样细胞百分比为(93.5±4.7)%。[2]
方法:食蟹猴胚胎干细胞 cyES 常规传代或用 Y-27632 (1-10 μM) 处理 24 h,使用 Flow Cytometry 方法进行活-死染色,使用试剂盒检测 BrdU。
结果:Y-27632 促进 cyES 存活细胞增加。Y-27632 没有促进细胞增殖,但保护细胞在单细胞消化后免于细胞死亡。[3]
体内活性 方法:为研究 Y-27632 在运动神经元疾病的治疗潜力,将 Y-27632 (2 or 30 mg/kg in drinking water) 口服给 ALS 模型的 SOD1G93A 小鼠,持续 137 天。
结果:Y-27632 2 mg/kg 治疗的效果不佳,Y-27632 30 mg/kg 治疗可改善雄性小鼠的运动功能,雌性小鼠仅表现出有限的改善。[4]
方法:为研究 Y-27632 对肝纤维化的影响,将 Y-27632 (30 mg/kg) 口服给药给 dimethylnitrosamine (DMN) 诱导肝纤维化的大鼠,每天一次,持续四周。
结果:Y-27632 治疗显著减少了 DMN 诱导的肝纤维化的发生,并降低了肝脏中胶原和羟脯氨酸的含量以及 α-SMA 的表达。[5]
激酶实验 Recombinant ROCK1/2, PKN, or citron kinase is expressed in HeLa cells as Myc-tagged proteins by transfection using Lipofectamine and is precipitated from the cell lysates by the use of 9E10 monoclonal anti-Myc antibody coupled to G protein-Sepharose. Recovered immunocomplexes are incubated with various concentrations of [32P]ATP and 10 mg of histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 30 min in a total volume of 30 μL of the kinase buffer containing 50 mM HEPES-NaOH, pH 7.4, 10 mM MgCl2, 5 mM MnCl2, 0.02% Briji 35, and 2 mM dithiothreitol. PKCa is incubated with 5 μM [32P]ATP and 200 μg/mL histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 10 min in a kinase buffer containing 50 mM Tris-HCl, pH 7.5, 0.5 mM CaCl2, 5 mM magnesium acetate, 25 μg/mL phosphatidylserine, 50 ng/mL 12-O-tetradecanoyl phorbol-13-acetate and 0.001% leupeptin in a total volume of 30 μL. Incubation is terminated by the addition of 10 μL of 43 Laemmli sample buffer. After boiling for 5 min, the mixture is subjected to SDS-polyacrylamide gel electrophoresis on a 16% gel. The gel is stained with Coomassie Brilliant Blue and then dried. The bands corresponding to histone type 2 are excised, and the radioactivity is measured [1].
细胞实验 HeLa cells are plated at a density of 3×10^4 cells per 3.5-cm dish. The cells are cultured in DMEM containing 10% FBS in the presence of 10 mM Thymidine for 16 h. After the cells are washed with DMEM containing 10% FBS, they are cultured for an additional 8 h, and then 40 ng/mL of Nocodazole is added. After 11.5 h of the Nocodazole treatment, various concentrations of Y-27632 (0-300 μM) or vehicle is added and the cells are incubated for another 30 min [1].
动物实验 A group of animals was injected with a single dose of pentylenetetrazole (PTZ, 65?mg/kg) to investigate if the two Rho-kinase inhibitors, fasudil, and Y-27632, changed the onset of PTZ seizures. Fasudil, Y-27632 or saline was given intraperitoneally 30?min before the PTZ injection. Each mouse was then observed for a 15-min period to measure the onset of the first myoclonic jerk, the onset of the first clonic convulsion and the occurrence of tonic hindlimb extension. Some of the animals died after tonic hindlimb extension, which is an expected outcome of acute PTZ injection. After the observation period, all animals were killed by halothane anesthesia [5]. Seven-week-old male Wistar rats were anesthetized with sodium pentobarbital. A silver clip (0.2 mm in diameter) was placed on the left renal artery in the preparation of the renal hypertensive rats. In the preparation of the DOCA-salt hypertensive rats, the left kidney was removed and a DOCA pellet (50 mg) was implanted subcutaneously. The DOCA rats were then fed an 8% salt diet. Rats from both groups were used after 8 weeks in the experiments, together with a male, 17–22-week old spontaneously hypertensive rats. The average systolic pressure in these groups of hypertensive rats ranged from 209 to 237 mm Hg, and no significant difference was found between groups. Eight-week-old male Wistar rats were used as controls. Their average systolic pressure was 139 mm Hg. Y-27632was administered orally. The systolic blood pressure was measured by the tail cuff method at 1, 3, 5, 7 and 24 h. The rats were prewarmed to 40 8C for 10 min before each measurement. No toxicity was found in rats treated with 30 mg kg?1 of Y-27632 administered per os once per day for 10 days [4].
别名 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐, Y-27632 2HCl
化合物与蛋白结合的复合物

T1870_1

The Catalytic Subunit of cAMP-dependent Protein Kinase (PKA) in Complex with Rho-kinase Inhibitor Y-27632

分子量 320.26
分子式 C14H21N3O·2HCl
CAS No. 129830-38-2

存储

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (156.12 mM)

H2O: 43.7 mM

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.1225 mL 15.6123 mL 31.2246 mL 78.0616 mL
5 mM 0.6245 mL 3.1225 mL 6.2449 mL 15.6123 mL
10 mM 0.3122 mL 1.5612 mL 3.1225 mL 7.8062 mL
20 mM 0.1561 mL 0.7806 mL 1.5612 mL 3.9031 mL
DMSO 50 mM 0.0624 mL 0.3122 mL 0.6245 mL 1.5612 mL
100 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7806 mL

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TargetMol Library Books参考文献

1. Wu Y, et al. ROCK inhibitor Y27632 promotes proliferation and diminishes apoptosis of marmoset induced pluripotent stem cells by suppressing expression and activity of caspase 3. Theriogenology. 2016 Jan 15;85(2):302-14. 2. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells. Chin Med J (Engl). 2012 Sep;125(18):3332-5. 3. Takehara T, et al. Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells. Mol Hum Reprod. 2008 Nov;14(11):627-34. 4. Günther R, et al. The rho kinase inhibitor Y-27632 improves motor performance in male SOD1(G93A) mice. Front Neurosci. 2014 Oct 7;8:304. 5. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36. 6. Schenke M, Schjeide B M, Püschel G P, et al. Analysis of Motor Neurons Differentiated from Human Induced Pluripotent Stem Cells for the Use in Cell-Based Botulinum Neurotoxin Activity Assays[J]. Toxins. 2020, 12(5): 276. 7. Chen X, Lin J, Hu T, et al. Galectin‐3 exacerbates ox‐LDL‐mediated endothelial injury by inducing inflammation via integrin β1‐RhoA‐JNK signaling activation[J]. Journal of cellular physiology. 2019 Jul;234(7):10990-11000. 8. Li Z, Luo W, Fang S, et al. Prostacyclin facilitates vascular smooth muscle cell phenotypic transformation via activating TP receptors when IP receptors are deficient[J]. Acta Physiologica. 2020: e13555. 9. Zhu Y, Wang L, Yu H, et al. In situ generation of human brain organoids on a micropillar array[J]. Lab on a Chip. 2017 Aug 22;17(17):2941-2950. 10. Gong-Bo Fu, Wei-Jian Huang, Min Zeng, Xu Zhou, Hong-Ping Wu, Chang-Cheng Liu, Han Wu, Jun Weng, Hong-Dan Zhang, Yong-Chao Cai, Charles Ashton, Min Ding, Dan Tang, Bao-Hua Zhang, Yi Gao, Wei-Feng Yu, Bo Zhai, Zhi-Ying He, Hong-Yang Wang, and He-Xin Yan . Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens [J]. Cell Research. 2019 Jan;29(1):8-22.

TargetMol Library Books文献引用

1. Fu G B, Huang W J, Zeng M, et al. Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens. Cell Research. 2019, 29(1): 8-22 2. Zhu Y, Wang L, Yu H, et al. In situ generation of human brain organoids on a micropillar array. Lab on A Chip. 2017 Aug 22;17(17):2941-2950 3. Wen L, Miao Y, Fan Z, et al. Establishment of an Efficient Primary Culture System for Human Hair Follicle Stem Cells Using the Rho-Associated Protein Kinase Inhibitor Y-27632. Frontiers in Cell and Developmental Biology. 2021 Mar 5;9:632882. doi: 10.3389/fcell.2021.632882. eCollection 2021. 4. Li Z, Luo W, Fang S, et al. Prostacyclin facilitates vascular smooth muscle cell phenotypic transformation via activating TP receptors when IP receptors are deficient. Acta Physiologica. 2020: e13555 5. Chen X, Lin J, Hu T, et al. Galectin‐3 exacerbates ox‐LDL‐mediated endothelial injury by inducing inflammation via integrin β1‐RhoA‐JNK signaling activation. Journal of Cellular Physiology. 2019 Jul;234(7):10990-11000 6. Schenke M, Schjeide B M, Püschel G P, et al. Analysis of Motor Neurons Differentiated from Human Induced Pluripotent Stem Cells for the Use in Cell-Based Botulinum Neurotoxin Activity Assays. Toxins. 2020, 12(5): 276 7. Zhu Y, Wang L, Yin F, et al. A hollow fiber system for simple generation of human brain organoids. Integrative Biology. 2017 Sep 18;9(9):774-781 8. Wang C, Li Y, Jia L, et al. CD276 expression enables squamous cell carcinoma stem cells to evade immune surveillance. Cell Stem Cell. 2021 Sep 2;28(9):1597-1613.e7. doi: 10.1016/j.stem.2021.04.011. Epub 2021 May 3. 9. Xu L, Kan S, Yu X, et al.Deep learning enables stochastic optical reconstruction microscopy-like superresolution image reconstruction from conventional microscopy.iScience.2023, 26(11). 10. Mergani A E, Meurer M, Wiebe E, et al.Alteration of cholesterol content and oxygen level in intestinal organoids after infection with Staphylococcus aureus.The FASEB Journal.2023, 37(12): e23279.
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Cucurbitacin A Belumosudil CID-5056270 ROCK-IN-7 BDP5290 ROCK-IN-6 Rho-Kinase-IN-1 CCG-232964

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 TGF-β/Smad靶点化合物库 抗癌活性化合物库 激酶抑制剂库 高选择性抑制剂库 人代谢物化合物库 抗衰老化合物库 细胞周期化合物库 细胞重编程化合物库 口服活性化合物库

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Keywords

Y-27632 dihydrochloride 129830-38-2 Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK pluripotent orally Y 27632 Dihydrochloride Y-27632 Dihydrochloride active 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐 inhibit Y-27632 2HCl epithelial-mesenchymal Y27632 Dihydrochloride Y27632 dihydrochloride Rho-kinase ROK ATP-competitive Rho-associated kinase modulation lineage transition-like stem cells Inhibitor Y 27632 mesendodermal Rho-associated protein kinase hIPSCs Y-27632 Y27632 Y 27632 dihydrochloride inhibitor

 

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