2. Membrane Transporter/Ion Channel Apoptosis Metabolic Enzyme/Protease
  3. P2X Receptor Apoptosis Farnesyl Transferase
  4. Minodronic acid

Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.

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Minodronic acid

Minodronic acid Chemical Structure

CAS No. : 180064-38-4

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Based on 1 publication(s) in Google Scholar

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Minodronic acid Related Antibodies

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1 Publications Citing Use of MCE Minodronic acid

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Description

Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer[1][2].

IC50 & Target

P2X2 Receptor

 

P2X3 Receptor

 

Cellular Effect
Cell Line Type Value Description References
HFF IC50
1.88 μM
Compound: 4
In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)
In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)
[PMID: 15857119]
J774 IC50
3 μM
Compound: 4
Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by alamar blue assay
Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by alamar blue assay
[PMID: 20394422]
T-cell IC50
4.1 μM
Compound: 3
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
[PMID: 14711309]
T-cell IC50
8 μM
Compound: 3
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
[PMID: 14711309]
In Vitro

Minodronic acid (5-100 μM; 72 h) inhibits the proliferation of human bladder cancer cell lines 253J, 5637, RT4, RT112, TCCSUP, KU-7 and UM-UC-3 in a dose-dependent manner[1].
Minodronic acid (30 μM; 48 h) induces apoptosis in human bladder cancer cells[1].
Minodronic acid (0.25-2.0 × IC50; 72 h) exhibits synergistic or additive antiproliferative effects when combined with Cisplatin (HY-17394) or Paclitaxel (HY-B0015) in human bladder cancer cell lines KU-7, RT112 and UM-UC-3[1].
Minodronic acid (0.1-1 μM; 3 days) potently inhibits osteoclast-mediated bone resorption in rabbits and induces dose-dependent morphological changes; at 1 μM, it almost completely inhibits bone resorption and causes osteoclast detachment, while at 0.1 μM, it only exerts partial inhibitory effects accompanied by the disappearance of the ruffled border[2].

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

Minodronic acid Related Antibodies

Cell Proliferation Assay[1]

Cell Line: 253J, 5637, RT4, RT112, TCCSUP, KU-7, UM-UC-3 human bladder cancer cells
Concentration: 5, 10, 25, 50, 100 μM
Incubation Time: 72 h
Result: Inhibited cell growth in a dose-dependent manner.
Achieved IC50 values of 12.2 μM (253J), 7.1 μM (5637), 12.2 μM (RT4), 15.4 μM (RT112), 21.8 μM (TCCSUP), 24.8 μM (KU-7), and 20.8 μM (UM-UC-3).
In Vivo

Minodronic acid (80 μg/kg; subcutaneous injection; once weekly; for 3 consecutive weeks) significantly inhibits the growth of bladder cancer bone metastases in BALB/c nu/nu mice without causing adverse effects[1].
Minodronic acid (30-100 μM; transurethral administration; 5 days) inhibits the growth of orthotopic bladder cancer in SCID mice [1].
Minodronic acid (0.05-5 mg/kg; subcutaneous injection; single administration) accumulates in the calcified and ossified regions of rat bones, concentrates in osteoclast-containing bone tissue sites, and exhibits dose-dependent bone tissue localization characteristics[2].

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

Animal Model: BALB/c nu/nu (female, 6-8 weeks old, intracardiac injection of 1×106 UM-UC-3^LUC cells to induce bone metastases)[1]
Dosage: 80 μg/kg
Administration: s.c.; once weekly; 3 weeks
Result: Significantly reduced growth of bone metastatic lesions compared to untreated mice.
Did not significantly inhibit visceral metastases.
Showed no significant differences in body weight or serum components (AST, ALT, LDH, TP, BUN, Cre, Ca) compared to untreated mice.
Animal Model: SCID (female, 6-8 weeks old, orthotopic implantation of 2×106 UM-UC-3^LUC cells into bladder)[1]
Dosage: 30 μM; 100 μM
Administration: transurethral; daily for 5 consecutive days (days 5-9)
Result: Significantly suppressed orthotopic bladder tumor growth, no significant systemic toxicity was observed, and occasional deaths were attributed to mechanical renal injury rather than drug-related toxicity.
Animal Model: F334/DuCrj rats (female, 4 days postpartum, 5-7 g)[2]
Dosage: 0.05 mg/kg (0.311 MBq/kg); 0.5 mg/kg (3.11 MBq/kg); 5 mg/kg (31.1 MBq/kg)
Administration: s.c.; single dose
Result: Localized approximately 2% of total administered radioactivity to right humeri at 24 hours post-administration, with radioactivity increasing linearly with dose.
Showed radioactive silver grains distributed in the calcified zone, ossification zone, and spongiosa of femurs, but absent in the hypertrophic cartilage zone.
Detected condensed silver grains in spongiosa under and surrounding osteoclasts, with low levels of intracellular silver grains present in osteoclasts.
Molecular Weight

322.15

Formula

C9H12N2O7P2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(P(O)(O)=O)(P(O)(O)=O)CC1=CN=C2C=CC=CN21
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 5 mg/mL (15.52 mM; Need ultrasonic and warming)

H2O : 5 mg/mL (15.52 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 80°C)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1041 mL 15.5207 mL 31.0414 mL
5 mM 0.6208 mL 3.1041 mL 6.2083 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 2 mg/mL (6.21 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / H2O 1 mM 3.1041 mL 15.5207 mL 31.0414 mL 77.6036 mL
5 mM 0.6208 mL 3.1041 mL 6.2083 mL 15.5207 mL
10 mM 0.3104 mL 1.5521 mL 3.1041 mL 7.7604 mL
15 mM 0.2069 mL 1.0347 mL 2.0694 mL 5.1736 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Minodronic acid Related Classifications

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:

Minodronic acid180064-38-4YM-529YM529YM 529P2X ReceptorApoptosisFarnesyl TransferaseP2XRsFtaseosteoporosisbladder cancerfarnesyl pyrophosphate synthasepurinergic P2X2/3 receptorsRasmouse modelsosteoclastsUM-UC-3 human bladder cancer cells253J human bladder cancer cellsRap1AInhibitorinhibitorinhibit

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