StemRegenin 1 (SR1)
(Synonyms: SR1) 目录号 : GC17043
StemRegenin 1 (SR1)是一种强效芳香烃受体（AhR）拮抗剂（IC50 = 127nM）。
Cas No.:1227633-49-9
Sample solution is provided at 25 µL, 10mM.
StemRegenin 1 (SR1) is a potent aromatic hydrocarbon receptor (AhR) antagonist (IC50 = 127nM) [1]. StemRegenin 1 promotes the self-renewal of human CD34⁺ hematopoietic stem cells (HSCs/HSPCs) by inhibiting aromatic receptors, and can also promote the differentiation of pluripotent stem cells (iPSCs) into hematogenous progenitor cells [2-3]. StemRegenin 1 can serve as a potential mitigator for radiation-induced hematopoietic system damage [4].
In multipotent hematopoietic progenitors, High-dose StemRegenin 1 (1-10µM; 7d) inhibits cell proliferation [5]. In human endothelial progenitor cells, StemRegenin 1 (1µM; 48h) delays endothelial progenitor cell senescence by regulating AhR pathway-mediated CYP1A1 and ROS generation [6].
In lethally irradiated mice model, treatment with StemRegenin 1 (30µg/kg; ip; 30d) significantly reduces mortality from total body irradiation [7]. In ovariectomized-induced bone loss mouse model, StemRegenin 1 (2.5mg/kg; ip; 42d) inhibits ovariectomy-induced bone loss in vivo [8].
References:
[1]. Boitano A E, Wang J, Romeo R, et al. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells[J]. Science, 2010, 329(5997): 1345-1348.
[2]. Kanashiro M A, Paul S K, Sone M, et al. iPSC-Derived Mesenchymal Stem Cells Supports the Ex Vivo expansion of Human Hematopoietic Stem and Progenitor Cells Via Sterile Inflammation Pathway[J]. Blood, 2023, 142: 2680.
[3]. Singh J, Chen E L Y, Xing Y, et al. Generation and function of progenitor T cells from StemRegenin-1–expanded CD34+ human hematopoietic progenitor cells[J]. Blood advances, 2019, 3(20): 2934-2948.
[4]. Guan D, Yang Y, Pang M, et al. Indole-3-carboxaldehyde ameliorates ionizing radiation-induced hematopoietic injury by enhancing hematopoietic stem and progenitor cell quiescence[J]. Molecular and cellular biochemistry, 2024, 479(2): 313-323.
[5]. Tao L, Togarrati P P, Choi K D, et al. StemRegenin 1 selectively promotes expansion of multipotent hematopoietic progenitors derived from human embryonic stem cells[J]. Journal of Stem Cells & Regenerative Medicine, 2017, 13(2): 75.
[6]. Lim H J, Jang W B, Rethineswaran V K, et al. StemRegenin-1 attenuates endothelial progenitor cell senescence by regulating the AhR pathway-mediated CYP1A1 and ROS generation[J]. Cells, 2023, 12(15): 2005.
[7]. Hwang Y J, Shin D Y, Kim M J, et al. StemRegenin 1 mitigates radiation-mediated hematopoietic injury by modulating radioresponse of hematopoietic stem/progenitor cells[J]. Biomedicines, 2023, 11(3): 824.
[8]. Zhou S, Li J, Ying T, et al. StemRegenin 1 attenuates the RANKL-induced osteoclastogenesis via inhibiting AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway[J]. Iscience, 2024, 27(5).
StemRegenin 1 (SR1)是一种强效芳香烃受体（AhR）拮抗剂（IC50 = 127nM） [1]。StemRegenin 1通过抑制芳香烃受体促进人类CD34⁺造血干细胞（HSC/HSPC）的自我更新，并能促进多能干细胞（iPSC）分化为造血祖细胞 [2-3]。StemRegenin 1可作为缓解辐射诱导的造血系统损伤的潜在药物 [4]。
在多能造血祖细胞中，高剂量StemRegenin 1（1-10µM；7d）可抑制细胞增殖 [5]。在人类内皮祖细胞中，StemRegenin 1（1µM；48h）通过调节AhR通路介导的CYP1A1和ROS生成来延缓内皮祖细胞衰老 [6]。
在致死性辐射小鼠模型中，StemRegenin 1（30µg/kg；ip；30d）治疗显著降低了全身辐射造成的死亡率 [7]。在卵巢切除诱发的骨质疏松小鼠模型中，StemRegenin 1（2.5mg/kg；ip；42d）可抑制卵巢切除诱发的体内骨质疏松 [8]。
| Cell experiment [1]: | |
Cell lines | Multipotent hematopoietic progenitors (MPs) |
Preparation Method | Lin-CD34+CD43+CD235a/CD41a- MPs were plated in duplicate in 96-well plates containing 4x103 cells/well. Cells were cultured in serum-free medium containing 10%BIT, 100µM 2-mercaptoethanol, and ExCyte in IMDM supplemented with 10ng/mL IL3, and 50ng/mL IL6 and SCF. StemRegenin 1 was added to the cultures at concentrations ranging from 1, 5 and 10µM. Viable cell count was determined using trypan blue. |
Reaction Conditions | 1-10µM; 7d |
Applications | High-dose StemRegenin 1 inhibits cell proliferation. |
| Animal experiment [2]: | |
Animal models | Lethally irradiated mice model |
Preparation Method | The C57BL/6 mice (male, 6–8 weeks) were purchased. Radiation exposure (1.0Gy/min) was performed as a single lethal dose of total body irradiation (TBI) using the X-RAD 320 device. To assess the efficacy of StemRegenin 1, TBI-exposed mice (6Gy, n = 10/group) were injected at 4h post-TBI with 100uL of normal saline or StemRegenin 1 (30µg/kg) via intraperitoneal injection. Survival was monitored for 30 days following irradiation. |
Dosage form | 30µg/kg; ip; 30d |
Applications | Treatment with StemRegenin 1 significantly reduces mortality from total body irradiation. |
References: | |
| Cas No. | 1227633-49-9 | SDF | |
| 别名 | SR1 | ||
| 化学名 | 4-[2-[[2-(1-benzothiophen-3-yl)-9-propan-2-ylpurin-6-yl]amino]ethyl]phenol | ||
| Canonical SMILES | CC(C)N1C=NC2=C1N=C(N=C2NCCC3=CC=C(C=C3)O)C4=CSC5=CC=CC=C54 | ||
| 分子式 | C24H23N5OS | 分子量 | 429.54 |
| 溶解度 | ≥ 21.5mg/mL in DMSO, ≥ 3.41 mg/mL in EtOH with ultrasonic | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3281 mL | 11.6404 mL | 23.2807 mL |
| 5 mM | 0.4656 mL | 2.3281 mL | 4.6561 mL |
| 10 mM | 0.2328 mL | 1.164 mL | 2.3281 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。
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