Olpadronic acid (Synonyms: Olpadronate; OLP)

Cat. No.: HY-106431 Purity: 95.0%: Data Sheet
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Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis.

For research use only. We do not sell to patients.

Olpadronic acid Chemical Structure

CAS No. : 63132-39-8

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Olpadronic acid:

Olpadronic acid (Standard) Get quote

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
T-cell	IC₅₀	112 μM Compound: 31	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]
T-cell	IC₅₀	46 μM Compound: 31	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]
Vero	IC₅₀	>200 μM Compound: 19	Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum	[PMID: 11300872]

In Vitro

Olpadronic acid (5 × 10^-8-10^-4 M) potently inhibits bone resorption in foetal mouse bone assays with a CI₅₀ of 5 × 10^-7 M^[1].
Olpadronic acid inhibits breast cancer cell adhesion to bone matrices^[1].

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

In Vivo

Olpadronate prevents and reverses osteopaenia across multiple mouse models^[1].
Olpadronate maintains and restores mechanical bone quality in rats with immobilisation- or ovariectomy-induced osteopaenia^[1].
Olpadronate (90 mg/kg/day; p.o.; long-term) improves the biomechanical strength of long bones in normal mice without impairing bone mineralisation^[1].
Olpadronate enhances the anabolic bone effects of simultaneous hPTH administration in normal rats by inhibiting remodelling of newly formed bone^[1].
Olpadronic acid (4-16 ug/100g; i.p.; once weekly; 30 days) prevents Cyclosporine-induced high bone resorption and trabecular bone loss in male Sprague-Dawley rats^[2].
Olpadronate (2.6 mmol/L; i.v.; 3 doses total) prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model^[3].

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

Animal Model:	Mice^[1]
Dosage:	90 mg/kg/day
Administration:	p.o.; long-term
Result:	Improved the resistance of long bones to deformation and fracture. Increased external diameter and diaphyseal moments of inertia for flexion and torsion. Did not impair matrix calcification.

Animal Model:	Sprague-Dawley rats (male, ~5 months old, 250-300 g, cyclosporine-induced osteopenia)^[2]
Dosage:	4; 8; 16 ug/100g rat
Administration:	i.p.; once weekly; 30 days
Result:	Caused a transient, statistically significant increase in serum bone-alkaline phosphatase (b-ALP) on day 14 in groups receiving 8 ug/100g and 16 ug/100g, and a significant reduction in serum b-ALP on day 30 compared to control and cyclosporine-only groups. Significantly reduced urinary deoxypyridinoline (DPyr) excretion on days 14 and 30 compared to cyclosporine-only rats, with the 16 ug/100g dose causing a greater reduction than the lower doses. Significantly increased BMD in the total skeleton, whole femur, lumbar spine, and proximal tibia on day 30 compared to control and cyclosporine-only rats. Resulted in significantly higher proximal tibia, whole femur, and lumbar spine BMD with the 16 ug/100g dose compared to the lower olpadronic acid doses. Showed no significant effects on middle tibia BMD with any dose.

Animal Model:	NCR nude (nu/nu) mice (6-month-old male, immunocompromised, intratibial inoculation with PC-3-GFP human prostate cancer cells)^[3]
Dosage:	2.6 mmol/L
Administration:	i.v.; 3 times total (1 month pre-implantation, at implantation, and 30 days post-implantation)
Result:	Prevented tumor volume from exceeding 1 cm³. Reduced GFP tumor area by 66% compared to tumor-bearing control mice. Reduced mean X-ray score to 0.9, with 8 of 19 mice showing no tibial abnormalities and 11 showing only minor abnormalities, representing a dramatic reduction in bone lesion severity that was significantly greater than that seen with pamidronate. Reduced serum calcium to 10.7 mg/dL compared to tumor-bearing control mice. Reduced serum parathyroid hormone-related protein (PTHrP) to 110 pg/mL compared to tumor-bearing control mice. Reduced serum osteoprotegerin to 58 pg/mL compared to tumor-bearing control mice.

Clinical Trial

Molecular Weight

263.12

Formula

C₅H₁₅NO₇P₂

CAS No.

63132-39-8

Appearance

Solid

Color

White to off-white

SMILES

O=P(O)(C(CCN(C)C)(P(O)(O)=O)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

H2O : 50 mg/mL (190.03 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.8005 mL	19.0027 mL	38.0055 mL
5 mM	0.7601 mL	3.8005 mL	7.6011 mL
10 mM	0.3801 mL	1.9003 mL	3.8005 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 95.0%

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Data Sheet (280 KB) SDS (393 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. Roldán EJ, et al Olpadronate: a new amino-bisphosphonate for the treatment of medical osteopathies. Expert Opin Investig Drugs. 1998 Sep;7(9):1521-38. [Content Brief]

[2]. Zeni SN, et al. Olpadronate prevents the bone loss induced by cyclosporine in the rat. Calcif Tissue Int. 2002 Jan;70(1):48-53. [Content Brief]

[3]. Yang M, et al. The bisphosphonate olpadronate inhibits skeletal prostate cancer progression in a green fluorescent protein nude mouse model. Clin Cancer Res. 2006 Apr 15;12(8):2602-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H2O	1 mM	3.8005 mL	19.0027 mL	38.0055 mL	95.0137 mL
	5 mM	0.7601 mL	3.8005 mL	7.6011 mL	19.0027 mL
	10 mM	0.3801 mL	1.9003 mL	3.8005 mL	9.5014 mL
	15 mM	0.2534 mL	1.2668 mL	2.5337 mL	6.3342 mL
	20 mM	0.1900 mL	0.9501 mL	1.9003 mL	4.7507 mL
	25 mM	0.1520 mL	0.7601 mL	1.5202 mL	3.8005 mL
	30 mM	0.1267 mL	0.6334 mL	1.2668 mL	3.1671 mL
	40 mM	0.0950 mL	0.4751 mL	0.9501 mL	2.3753 mL
	50 mM	0.0760 mL	0.3801 mL	0.7601 mL	1.9003 mL
	60 mM	0.0633 mL	0.3167 mL	0.6334 mL	1.5836 mL
	80 mM	0.0475 mL	0.2375 mL	0.4751 mL	1.1877 mL
	100 mM	0.0380 mL	0.1900 mL	0.3801 mL	0.9501 mL

Olpadronic 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:

Olpadronic acid63132-39-8Olpadronate OLPFarnesyl TransferaseFtasebone metastasesDictyostelium discoideumPaget’s bone diseaseosteoporosishPTHmitochondrial myopathyprostate cancer cellosteoclastosteogenesis imperfectahypercalcaemia of malignancyInhibitorinhibitorinhibit

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