1. GPCR/G Protein
  2. RXFP Receptor
  3. RXFP2 agonist 2

RXFP2 agonist 2 是一种选择性,具有口服活性的 RXFP2 变构激动剂,EC50 值为 0.38 µM。RXFP2 agonist 2 诱导成骨细胞矿化。RXFP2 agonist 2 增加雌性小鼠的骨形成。RXFP2 agonist 2 具有研究骨质疏松症的潜力。

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RXFP2 agonist 2 Chemical Structure

RXFP2 agonist 2 Chemical Structure

CAS No. : 2971704-85-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RXFP2 agonist 2 is a selective,orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis[1].

IC50 & Target

EC50: 0.38 µM (RXFP2)[1]

体外研究
(In Vitro)

RXFP2 agonist 2 (Compound 6641) (1, 3, 5 µM; 14 天) 在 3 和 5 µM 诱导成骨细胞矿化,对 HCO 细胞无细胞毒性[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: HCO cells
Concentration: 0-100 µM
Incubation Time: 14 days
Result: Induced mineralization of primary human osteoblasts and is non-cytotoxic.
体内研究
(In Vivo)

RXFP2 agonist 2 (10 mg/kg; p.o.; 每周 3 次,8 周) 促进雌性小鼠骨形成[1]

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

Animal Model: 8-week-old WT C57BL/6 J female mice[1]
Dosage: 3 mg/kg for i.v.; 10 mg/kg for p.o.
Administration: I.v. or p.o.
Result: Exhibited a half-life of between 4-6.5 h depending on the route of administration, with no accumulation at 10 mg/kg, and oral bioavailability around 25-31%.
Animal Model: 8-week-old WT C57BL/6 J female mice[1]
Dosage: 10 mg/kg
Administration: P.o.; 3 times per week for 8 weeks
Result: Increased bone formation in mouse with significantly increased in Tb.N and Tb.Th, and increased BV/TV and decreased Tb.Sp.
分子量

787.37

Formula

C29H19F9IN3O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

RXFP2 agonist 2 相关分类

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  • 稀释计算器

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  • 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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RXFP2 agonist 2
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HY-150186
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