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DIPQUO

Cat No.:V33363 Purity: ≥98%
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP) with EC50 of 6.27 μM in C2C12 cells.
DIPQUO
DIPQUO Chemical Structure CAS No.: 1269365-82-3
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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5mg
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Product Description
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP) with EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes osteoblast differentiation in mice and humans by activating p38 MAPK-β.
DIPQUO is a small-molecule activator of the bone marker alkaline phosphatase (ALP). It promotes osteoblast differentiation in mice and humans by activating p38 MAPK-beta. DIPQUO has an EC50 of 6.27 microM in C2C12 cells. The compound markedly promotes osteoblast differentiation, including expression of Runx2, Osterix, and Osteocalcin. DIPQUO is a Wnt/beta-catenin signaling modulator that promotes osteogenic differentiation and bone formation. It is intended for laboratory research use only and has not been approved for human therapeutic use.
Biological Activity I Assay Protocols (From Reference)
Targets
DIPQUO targets the bone marker alkaline phosphatase (ALP), an enzyme that is essential for bone mineralization and is a key marker of osteoblast differentiation. The compound promotes osteoblast differentiation by activating p38 MAPK-beta, a member of the mitogen-activated protein kinase family. DIPQUO also modulates Wnt/beta-catenin signaling, a critical pathway in bone metabolism and osteogenic differentiation. The compound promotes the expression of osteogenic markers including Runx2, Osterix, and Osteocalcin. By activating these signaling pathways, DIPQUO mediates osteogenesis and promotes bone formation. Its mechanism of action involves the activation of p38-beta and modulation of Wnt signaling.
ln Vitro
DIPQUO demonstrates potent in vitro activity as an activator of alkaline phosphatase and osteoblast differentiation. The compound has an EC50 of 6.27 microM in C2C12 cells, a mouse myoblast cell line that can differentiate into osteoblasts. DIPQUO markedly promotes osteoblast differentiation, including expression of Runx2, Osterix, and Osteocalcin, mediating osteogenesis through activation of p38-beta. The compound promotes the differentiation of mouse and human osteoblasts by activating p38 MAPK-beta. DIPQUO's activity is concentration-dependent, with effects observed at micromolar concentrations. Its ability to promote osteogenic differentiation makes it a valuable tool for studying bone formation and metabolism.
ln Vivo
In vivo, DIPQUO has been studied for its effects on bone formation and osteogenic differentiation. As a Wnt/beta-catenin signaling modulator that promotes osteogenic differentiation and bone formation, DIPQUO has potential applications in bone regeneration and the treatment of bone disorders. The compound promotes osteoblast differentiation in mice and humans. Comprehensive in vivo efficacy data for DIPQUO have been reported in research publications. The compound's ability to activate p38 MAPK-beta and promote osteogenic differentiation supports its potential for bone-related therapeutic applications. DIPQUO serves as a valuable chemical probe for exploring the molecular mechanisms underlying bone metabolism and Wnt-driven tissue regeneration processes.
Enzyme Assay
In vitro enzyme assays for DIPQUO involve measuring the activation of alkaline phosphatase activity. Alkaline phosphatase activity is measured using a colorimetric assay with p-nitrophenyl phosphate as substrate. The enzyme is incubated with varying concentrations of the test compound, and the production of p-nitrophenol is measured spectrophotometrically. EC50 values are calculated from dose-response curves using non-linear regression analysis. The compound has an EC50 of 6.27 microM in C2C12 cells. Alternatively, osteoblast differentiation assays can be performed using C2C12 cells or primary osteoblasts, and ALP activity is measured as a marker of differentiation. Each concentration is typically tested in duplicate or triplicate. Positive controls (known osteogenic agents) and vehicle controls are included.
Cell Assay
In vitro cellular assays for DIPQUO are performed using osteoblast precursor cells such as C2C12 cells or primary osteoblasts. Cells are cultured in osteogenic differentiation medium and treated with varying concentrations of DIPQUO for 7-14 days. Alkaline phosphatase activity is measured using a colorimetric assay. Mineralization is assessed by alizarin red or von Kossa staining. Gene expression of osteogenic markers (Runx2, Osterix, Osteocalcin) is analyzed by qRT-PCR. The compound has an EC50 of 6.27 microM in C2C12 cells. Signaling pathway activation is assessed by Western blot for phosphorylated p38 MAPK. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. Results are expressed as fold-change in ALP activity or marker gene expression compared to vehicle-treated controls.
Animal Protocol
In vivo animal studies for DIPQUO are conducted using rodent models of bone formation and bone disorders. The compound is administered via intraperitoneal injection, subcutaneous injection, or oral gavage at various doses and schedules. Bone formation is assessed by micro-CT imaging to measure bone volume, trabecular thickness, and bone mineral density. Histomorphometry is performed on undecalcified bone sections to assess osteoblast number, bone formation rate, and mineralization. Serum markers of bone formation (P1NP) and resorption (CTX-1) are measured. Pharmacokinetic studies assess drug concentrations in plasma and bone tissue. Animals are monitored for clinical signs and body weight. Efficacy is expressed as improvement in bone parameters compared to vehicle-treated controls.
ADME/Pharmacokinetics
Pharmacokinetic properties of DIPQUO have been characterized in preclinical studies. The compound has a molecular formula of C20H17N3O and a molecular weight of 315.37 g/mol. It is soluble in DMSO (5 mg/mL with ultrasonic warming and heating to 60degC). Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of bone formation and metabolism. Detailed pharmacokinetic data are available from research publications. The compound's ability to reach bone tissue is a key consideration for its efficacy.
Toxicity/Toxicokinetics
DIPQUO is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a modulator of bone formation, the compound would be expected to have effects on bone metabolism. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported in the public domain. The compound is not approved for human use and is strictly intended for research purposes.
References

[1]. Discovery of a Small Molecule Promoting Mouse and Human Osteoblast Differentiation via Activation of p38 MAPK-β. Cell Chem Biol. 2019 Mar 29.

Additional Infomation
DIPQUO is an activator of alkaline phosphatase (ALP) with an EC50 of 6.27 microM in C2C12 cells. It promotes osteoblast differentiation by activating p38 MAPK-beta. DIPQUO promotes expression of Runx2, Osterix, and Osteocalcin. It is a Wnt/beta-catenin signaling modulator that promotes osteogenic differentiation and bone formation. The compound has a molecular formula of C20H17N3O and a molecular weight of 315.37 g/mol. DIPQUO has not entered clinical trials and has not received regulatory approval. It is available for research purposes only. DIPQUO is a valuable research tool for studying bone metabolism and developing new therapies for bone disorders.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H17N3O
Molecular Weight
315.368484258652
Exact Mass
315.137
CAS #
1269365-82-3
PubChem CID
50950764
Appearance
Light yellow to yellow solid powder
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
2
Heavy Atom Count
24
Complexity
511
Defined Atom Stereocenter Count
0
SMILES
O=C1C(C2=C(C3C=CC=CC=3)N=CN2)=CC2C=C(C)C=C(C)C=2N1
InChi Key
KTMBLNYSLKFCIR-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H17N3O/c1-12-8-13(2)17-15(9-12)10-16(20(24)23-17)19-18(21-11-22-19)14-6-4-3-5-7-14/h3-11H,1-2H3,(H,21,22)(H,23,24)
Chemical Name
6,8-dimethyl-3-(4-phenyl-1H-imidazol-5-yl)-1H-quinolin-2-one
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~5 mg/mL (~15.85 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 0.5 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 0.5 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1709 mL 15.8544 mL 31.7088 mL
5 mM 0.6342 mL 3.1709 mL 6.3418 mL
10 mM 0.3171 mL 1.5854 mL 3.1709 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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