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 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).

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MCB-22-174

MCB-22-174 Chemical Structure

CAS No. : 3058199-58-6

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MCB-22-174 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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Description

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].

In Vitro

MCB-22-174 (0-40 μM) exhibits potent agonistic activity on Piezo1 in C3H10T1/2 cells with an EC50 value of 6.28 μM[1].
MCB-22-174 (3-5 μM, 72 h) significantly upregulates the mRNA level of Runx2 in rMSCs and promotes osteogenesis more effectively than Yoda1 (HY-18723)[1].
MCB-22-174 (5 μM, 5-15 min) remarkably upregulates p-ERK and p-CaMKII in rMSCs, and activates the CaMKII/ERK signaling pathway more efficiently than Yoda1[1].
MCB-22-174 (5 μM) significantly decreases the expression of chondrogenesis markers (Comp, Acan) and adipogenesis markers (Lpl, Fabp4) in MSCs, showing a more significant suppression of chondrogenesis and adipogenesis than Yoda1[1].

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

MCB-22-174 Related Antibodies

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.
In Vivo

MCB-22-174 (2 mg/kg (5 μmol/kg), intraperitoneally injected on days 1, 4, 7, 10, and 13) can effectively improve bone quality in hind-limb unloading (HU) model rats[1].

MedChemExpress (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.
Molecular Weight

429.37

Formula

C16H14DCl2N5OS2
CAS No.
SMILES

ClC(C=CC=C1Cl)=C1C([2H])SC2=NN=C(C3=NC=C(NC[C@H](O)C)N=C3)S2
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Room temperature in continental US; may vary elsewhere.
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References
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MCB-22-174 Related Classifications

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    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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