2. Membrane Transporter/Ion Channel Others Stem Cell/Wnt MAPK/ERK Pathway Neuronal Signaling
  3. Piezo Channel Isotope-Labeled Compounds ERK CaMK
  4. MCB-22-174

MCB-22-174是一种氘代的 Piezo1 激动剂，其 EC50 为 6.28 μM。MCB-22-174 可显著激活大鼠骨髓间充质干细胞 (rMSCs) 中的 CaMKII/ERK 信号通路，并启动 Ca2+ 内流。MCB-22-174 能显著降低间充质干细胞 (MSCs) 中软骨形成标志物 (Comp、Acan) 和脂肪形成标志物 (Lpl、Fabp4) 的表达。MCB-22-174 能有效改善后肢去负荷 (HU) 模型大鼠的骨质量。MCB-22-174 可用于废用性骨质疏松 (OP) 的研究。

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MCB-22-174

MCB-22-174 Chemical Structure

CAS No. : 3058199-58-6

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MCB-22-174 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

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CaMK II CaMK III/eEF-2K CAMK IV PHK Trio DCAMKL

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MCB-22-174 is a deuterated Piezo1 agonist, with an EC50 value of 6.28 μM. MCB-22-174 remarkably activates the CaMKII/ERK signaling pathway and initiates Ca2+ influx in rMSCs. MCB-22-174 significantly decreases the expression of chondrogenesis markers (Comp, Acan) and adipogenesis markers (Lpl, Fabp4) in MSCs. MCB-22-174 can effectively improve bone quality in hind-limb unloading (HU) model rats. MCB-22-174 can be used for the study of disuse osteoporosis (OP)[1].

体外研究
(In Vitro)

MCB-22-174 (0-40 μM) 在 C3H10T1/2 细胞中对 Piezo1 表现出强效激动活性，其 EC50 为 6.28 μM[1]。
MCB-22-174 (3-5 μM, 72 h) 可显著上调大鼠骨髓间充质干细胞 (rMSCs) 中 Runx2 的 mRNA 水平，且比 Yoda1 (HY-18723) 更有效地促进成骨作用[1]。
MCB-22-174 (5 μM, 5-15 min) 能显著上调大鼠骨髓间充质干细胞 (rMSCs) 中的 p-ERK 和p-CaMKII，并比 Yoda1 更高效地激活 CaMKII/ERK 信号通路[1]。
MCB-22-174 (5 μM) 可显著降低间充质干细胞 (MSCs) 中软骨形成标志物 (Comp、Acan) 和脂肪形成标志物 (Lpl、Fabp4) 的表达，相比 Yoda1，对软骨形成和脂肪形成的抑制作用更显著[1]。

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

MCB-22-174 相关抗体:

Real Time qPCR[1]

Cell Line: rMSCs
Concentration: 3, 5 μM
Incubation Time: 72 h
Result: Upregulated the mRNA level of Runx2 in rMSCs.

Western Blot Analysis[1]

Cell Line: rMSCs
Concentration: 5 μM
Incubation Time: 5, 10, 15 min
Result: Upregulated p-ERK and p-CaMKII in rMSCs.
体内研究
(In Vivo)

MCB-22-174 (2 mg/kg (5 μmol/kg)，于第 1、4、7、10 和 13 天腹腔注射) 能有效改善后肢去负荷 (HU) 模型大鼠的骨质量[1]。

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

Animal Model: SD rats (2-month-old) were subjected to hind-limb unloading by tail suspension, with their tails fixed on the upper lids of cages to detach the hind limbs from the ground (forelimbs unaffected), simulating weightlessness to induce disuse osteoporosis[1]
Dosage: 2 mg/kg (5 μmol/kg)
Administration: Intraperitoneally injected on days 1, 4, 7, 10, and 13
Result: Improved bone quality in HU model rats.
Upregulated bone volume ratio (BV/TV) and trabecular thickness (Tb.Th.).
Downregulated trabecular separation (Tb.Sp.).
Increased the fluorescent area of alkaline phosphatase (ALP).
Promoted osteogenesis, with better efficacy than Yoda1.
分子量

429.37

Formula

C16H14DCl2N5OS2
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

MCB-22-174 相关分类

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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.

Keywords:

MCB-22-1743058199-58-6Piezo ChannelIsotope-Labeled CompoundsERKCaMKExtracellular signal regulated kinasesCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesdisuse osteoporosisCaMKIIPiezo1Inhibitorinhibitorinhibit

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