2. NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  3. RANKL/RANK Nuclear Factor of activated T Cells (NFAT) Cathepsin
  4. Y1693

Y1693 是一种口服有效的 RANKL 抑制剂，对 hRANKL 的 Kd=5.03 μM。Y1693 通过阻断其与 RANK 的相互作用抑制下游 c-fos/NFATc1 信号通路激活。Y1693 可显著抑制 RANKL 诱导的破骨细胞分化、F-actin 环形成及骨吸收活性，同时下调 TRAP、cathepsin K、c-fos 和 NFATc1 的 mRNA 及蛋白表达。Y1693 对骨髓来源巨噬细胞及破骨细胞前体细胞无明显细胞毒性，表现出良好的 ADME 特性。Y1693 能改善小鼠卵巢切除诱导的骨质疏松症，并逆转结扎诱导的牙周牙槽骨丢失。Y1693 可用于骨质疏松症与牙周疾病的相关研究。

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Y1693

Y1693 Chemical Structure

CAS No. : 2812381-74-9

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Y1693 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

查看所有亚型
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Y1693 is an orally active RANKL inhibitor with a Kd of 5.03 μM for hRANKL. Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP, cathepsin K, c-fos and NFATc1. Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases[1][2].

IC50 & Target

Cathepsin E

 

体外研究
(In Vitro)

Y1693 (0.1-10 μM; 5-6 d) 可强效抑制 RANKL 诱导的骨髓巨噬细胞 (BMMs) 破骨细胞生成，其 IC50 为 0.52 μM，在 1 μM 浓度下抑制率达 89.3%，在 0.1 μM 浓度下抑制率为 45.9%[1]。
Y1693 (1-10 μM; 3 d) 在浓度高达 10 μM 时对 BMMs 无细胞毒性[1]。
Y1693 (0.1-5 μM; 5-6 d) 可在体外以剂量依赖方式抑制 RANKL 诱导的骨髓巨噬细胞来源破骨细胞中 F-actin 环的形成[1]。
Y1693 (0.5-5 μM; 3 d) 可在 RANKL 刺激的骨髓巨噬细胞中呈剂量依赖性地下调 TRAP、组织蛋白酶 K、c-fos 和 NFATc1 的 mRNA 表达[1]。
Y1693 (1-10 μM; 3 d) 可呈剂量依赖性地抑制 RANKL 刺激的 BMM 中 c-fos 和 NFATc1 的蛋白表达[1]。
Y1693 (0.1-5 μM; 2 d) 可剂量依赖性地抑制成熟破骨细胞在牛股骨骨片上由 RANKL 诱导的骨吸收，在 5 μM 时几乎可完全抑制该过程[1]。

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

Y1693 相关抗体:

Cell Viability Assay[1]

Cell Line: bone marrow-derived macrophages (BMMs)
Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 3 day
Result: Showed no cytotoxicity to BMMs at concentrations up to 10 μM.
Maintained relative cell viability above 1.5-fold (similar to untreated controls) across all tested concentrations.

Real Time qPCR[1]

Cell Line: bone marrow-derived macrophages (BMMs)
Concentration: 0.5 μM, 1 μM, 2.5 μM, 5 μM
Incubation Time: 3 day
Result: Dose-dependently reduced the RANKL-induced upregulation of osteoclast marker genes.
Suppressed TRAP, cathepsin K, c-fos, and NFATc1 mRNA levels to near basal (unstimulated) levels at 5 μM.
Exhibited significant inhibition at concentrations as low as 0.5 μM.

Western Blot Analysis[1]

Cell Line: bone marrow-derived macrophages (BMMs)
Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 3 day
Result: Reduced the protein expression of c-fos and NFATc1 in a dose-dependent manner.
Showed decreasing protein levels as concentration increased from 1 μM to 10 μM.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t T1/2 CL Cmax F
Rat[1] 3 mg/kg i.v. 2710 ng·h/mL 5.1 h 18.6 mL/min/kg / /
Rat[1] 5 mg/kg p.o. 223 ng·h/mL 2.0 h / 48.1 ng/mL 4.9 %
体内研究
(In Vivo)

Y1693 (20-60 mg/kg；口服；每周 5 次、每日 1 次；连续 28 天) 可使骨质疏松症去卵巢小鼠的骨密度恢复 23.4%，并改善其骨丢失情况[1]。
Y1693 (20 mg/kg；腹腔注射；每日一次；持续 28 天) 可使小鼠牙槽骨量增加 60.7%、骨体积增加 51.9%，同时改善结扎诱导的小鼠牙周骨丢失[1]。

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

Animal Model: C57BL/6 mice with Osteoporosis (8-week-old female; ovariectomy-induced osteoporosis)[1]
Dosage: 20 mg/kg; 60 mg/kg
Administration: p.o.; once daily 5×/week; 28 days
Result: Increased bone mineral density by 23.4% compared to ovariectomized control mice.
Ameliorated osteoporosis-related bone loss.
Animal Model: BALB/C mice with Periodontal disease (8-week-old male; ligature-induced periodontal disease)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 28 days
Result: Increased alveolar bone mass by 60.7% compared to ligature-induced periodontal disease control mice.
Increased bone volume by 51.9% compared to ligature-induced periodontal disease control mice.
Increased vertical bone remaining at M2-M3 by 67.0% compared to ligature-induced periodontal disease control mice.
Preserved alveolar bone structure.
分子量

419.52

Formula

C28H25N3O
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

Y1693 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

Y16932812381-74-9Y 1693Y-1693RANKL/RANKNuclear Factor of activated T Cells (NFAT)Cathepsinc-fos/NFATc1 signaling pathwaybone marrow-derived macrophagesRANKLTNFαosteoporosismouse bone marrow osteoclast precursor cellsperiodontal diseaseF-actin ringosteoclastRANKInhibitorinhibitorinhibit

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