2. Membrane Transporter/Ion Channel Stem Cell/Wnt MAPK/ERK Pathway
  3. Piezo Channel ERK
  4. Piezo1 agonist 1-d2

Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis.

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Piezo1 agonist 1-d<sub>2</sub>

Piezo1 agonist 1-d2 Chemical Structure

CAS No. : 3058199-62-2

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Piezo1 agonist 1-d2 Related Antibodies

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Description

Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

IC50 & Target

EC50: 2.21 μM (Piezo1)
In Vitro

Piezo1 agonist 1-d2 (compound 12a) (0.125-32 μM; 2 h) potently activates Piezo1 and induces Ca2+ influx in C3H10T1/2 mesenchymal stem cells (MSCs), with an EC50 of 2.21 μM[1].
Piezo1 agonist 1-d2 (3-5 μM; 72 h) promotes osteogenesis of bone marrow mesenchymal stem cells (BMSCs) in a dose-dependent manner, and upregulates the expression of Runx2 and Osxm RNA[1].
Piezo1 agonist 1-d2 (5 μM; 5-15 min) activates the Erk signaling pathway in BMSCs[1].

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

Piezo1 agonist 1-d2 Related Antibodies

Real Time qPCR[1]

Cell Line: bone marrow mesenchymal stem cells (BMSCs)
Concentration: 3, 5 μM
Incubation Time: 72 h
Result: Significantly upregulated Runx2 mRNA levels at 3 μM, but did not significantly alter Osx mRNA levels.
Significantly upregulated both Runx2 mRNA levels and Osx mRNA levels at 5 μM.

Western Blot Analysis[1]

Cell Line: bone marrow mesenchymal stem cells (BMSCs)
Concentration: 5 μM
Incubation Time: 5, 10, 15 min
Result: Significantly increased p-Erk levels at 5 min.
Showed higher p-Erk/Erk ratios at 5, 10, and 15 min compared to vehicle control.
In Vivo

Piezo1 agonist 1-d2 (5 μM/kg; i.p.; 5 administrations) effectively alleviates disuse osteoporosis in hindlimb unloaded rats[1].

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

Animal Model: Sprague-Dawley (SD) (2 months old, hindlimb-unloading osteoporosis model)[1]
Dosage: 5 μM/kg
Administration: i.p.; 5 doses on days 1, 4, 7, 10, 13 after hindlimb unloading initiation
Result: Increased bone volume fraction (BV/TV), trabecular number (Tb.N.), and reduced trabecular separation (Tb.Sp.) compared to untreated hindlimb-unloading group.
Significantly increased Alp fluorescent area (osteogenic marker) relative to untreated hindlimb-unloading group, with osteogenesis levels nearly matching weight-bearing control rats.
Showed no significant liver or kidney toxic side effects during treatment.
Molecular Weight

430.37

Formula

C16H13D2Cl2N5OS2
CAS No.
SMILES

ClC1=C(C(Cl)=CC=C1)C([2H])(SC2=NN=C(S2)C3=CN=C(C=N3)NC[C@@H](C)O)[2H]
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Piezo1 agonist 1-d2 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

Piezo1 agonist 1-d23058199-62-2Piezo ChannelERKExtracellular signal regulated kinasesC3H10T1/2 MSCsmesenchymal stem cellsPiezo1liver microsomesOsxdisuse osteoporosishindlimb-unloading rat modelBMSCsRunx2Erk signaling pathwayInhibitorinhibitorinhibit

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