1. Immunology/Inflammation
  2. Aryl Hydrocarbon Receptor
  3. Stemregenin 1

Stemregenin 1 (SR1) (GMP) 是 GMP 级别的 Stemregenin 1 (HY-15001)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。Stemregenin 1 是一种有效的芳香烃受体 (AhR) 拮抗剂,IC50 为 127 nM。Stemregenin 1 (GMP) 可竞争性结合 AhR 并抑制其核转位,通过阻断 AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 信号通路,发挥抑制破骨细胞生成、促进造血祖细胞扩增的活性。Stemregenin 1 (GMP) 可用于骨质疏松治疗、造血干细胞体外扩增及骨代谢疾病机制研究。

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Stemregenin 1 Chemical Structure

Stemregenin 1 Chemical Structure

CAS No. : 1227633-49-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC50 of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the treatment of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases[1][2][3][4].

IC50 & Target

IC50: 127 nM (AhR)[4]

体外研究
(In Vitro)

Stemregenin 1 (GMP) (1、5、10 μM;7 天) 在人胚胎干细胞衍生的造血祖细胞实验中,可浓度依赖性促进 CD34+ 细胞扩增,增强集落形成能力,但 10 μM 时抑制细胞增殖[1]
Stemregenin 1 (GMP) (0.75 μM;7 天) 与 DMOG 联合在 CD34+ 脐带血细胞实验中,能增加原始造血亚群比例,提升长期集落形成单位数量[2]
Stemregenin 1 (GMP) (3、6、8、10 μM;4-7 天) 在骨髓巨噬细胞实验中,可抑制 RANKL 诱导的破骨细胞分化,减少 NFATc1、ACP5 等基因表达及 F-actin 环形成[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1][2][3]

Cell Line: BMMs, hESC-derived hematopoietic progenitors, CD34+ cord blood cells
Concentration: 0-10 μM
Incubation Time: 48-96 h for BMMs; 7 days for others
Result: Hed no cytotoxicity in BMMs at ≤10 μM, and maintained CD34+ cells viability without significant loss at 0.75 μM.
体内研究
(In Vivo)

Stemregenin 1 (GMP) (2.5 mg/kg;腹腔注射;每 3 天 1 次;42 天) 在小鼠卵巢切除 (OVX) 骨质疏松模型中,可逆转骨丢失,减少破骨细胞数量并增加骨密度[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (female, 8 weeks old, 20-25 g) with ovariectomized (OVX) osteoporosis model[3]
Dosage: 2.5 mg/kg
Administration: Intraperitoneal injection, once every 3 days, for 42 days
Result: Reversed OVX-induced bone loss, as shown by micro-CT analysis demonstrating increased trabecular bone volume/total volume (BV/TV).
Improved bone mineralization.
Serum markers of bone resorption were reduced, and bone formation markers were enhanced.
分子量

429.54

同用名

SR1

Formula

C24H23N5OS

CAS 号
性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

纯度 & 产品资料
参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Stemregenin 1
目录号:
HY-15001G
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