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Risedronate

CAS# 105462-24-6

Risedronate

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Chemical structure

Risedronate

3D structure

Chemical Properties of Risedronate

Cas No. 105462-24-6 SDF Download SDF
PubChem ID 5245 Appearance Powder
Formula C7H11NO7P2 M.Wt 283.11
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Risedronate
Solubility DMSO : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name (1-hydroxy-1-phosphono-2-pyridin-3-ylethyl)phosphonic acid
SMILES OC(Cc1cccnc1)([P](O)(O)=O)[P](O)(O)=O
Standard InChIKey IIDJRNMFWXDHID-UHFFFAOYSA-N
Standard InChI InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Risedronate

DescriptionRisedronic acid (Risedronate ) is a pyridinyl biphosphonate which inhibits osteoclast-mediated bone resorption. Target: Others Risedronate, which was promoted in Croatia a few months ago, is the latest (III) generation of bisphosphonates, the most efficient anti-resorption drugs that inhibit osteoclast-mediated bone resorption and change the bone metabolism. Risedronate is hence the first line of bisphosphonates for the reduction of vertebral and non-vertebral fracture risks in postmenopausal women with osteoporosis or those with a high risk of osteoporosis. It also efficiently prevents bone loss or improves bone density in men and women on a long-term corticosteroid therapy . The administration of 20 and 25 mg/kg risedronate for 4 days led to decreases of parasitemia of 68.9% and 83.6%, respectively. On the seventh day of treatment the inhibitions were 63% and 88.9% with 20 and 25 mg/kg, respectively. After recovering the parasitemia, a dose-response curve was obtained for estimating the ID50 (dose causing 50% inhibition), equivalent to 17 ± 1.8 mg/kg after 7 days of treatment. Four days after the interruption of treatment (11 days postinfection), the parasitemias of the groups treated with 10, 15, 20, and 25 mg/kg/day were 15.3%, 15.9%, 15.2%, and 5.7%, respectively. Conversely, the group that received PBS presented parasitemia of 25.6%. Among the groups treated with risedronate, only the animals that received 25 mg/kg had a significant inhibition of 77.8% (see Table S1 in the supplemental material), demonstrating that even after treatment discontinuation, the parasitemia of the animals remained low in relation to that of the controls .

References:
[1]. Giljevic Z, et al. Treatment of osteoporosis by risedronate-- speed, efficacy and safety. Reumatizam. 2006;53(2):66-71. [2]. Jordao FM, et al. In vitro and in vivo antiplasmodial activities of risedronate and its interference with protein prenylation in Plasmodium falciparum. Antimicrob Agents Chemother. 2011 May;55(5):2026-31.

Risedronate Dilution Calculator

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Risedronate Molarity Calculator

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Preparing Stock Solutions of Risedronate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5322 mL 17.661 mL 35.322 mL 70.6439 mL 88.3049 mL
5 mM 0.7064 mL 3.5322 mL 7.0644 mL 14.1288 mL 17.661 mL
10 mM 0.3532 mL 1.7661 mL 3.5322 mL 7.0644 mL 8.8305 mL
50 mM 0.0706 mL 0.3532 mL 0.7064 mL 1.4129 mL 1.7661 mL
100 mM 0.0353 mL 0.1766 mL 0.3532 mL 0.7064 mL 0.883 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Risedronate

Risedronic acid (Risedronate ) is a pyridinyl biphosphonate which inhibits osteoclast-mediated bone resorption.

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References on Risedronate

Risedronate therapy in patients with mild-to-moderate chronic kidney disease with osteoporosis: post-hoc analysis of data from the risedronate phase III clinical trials.[Pubmed:28201994]

BMC Nephrol. 2017 Feb 15;18(1):66.

BACKGROUND: The clinical effect of bisphosphonate treatment has not been clearly evaluated by kidney function in Japanese Chronic Kidney Disease (CKD) patients with osteoporosis. This study analyzed the data from three Risedronate Japanese phase III trials. The clinical effect of Risedronate therapy was evaluated in CKD patients with osteoporosis. METHODS: The Japanese clinical trials involved 852 subjects who received Risedronate (2.5 mg once daily or 17.5 mg once weekly) and whose estimated glomerular filtration rate (eGFR) were calculable and at >/= 30 mL/min. The subjects were divided into subgroups according to the eGFR level: >/= 90 mL/min/1.73 m(2), >/= 60 to < 90 mL/min/1.73 m(2), >/= 30 to < 60 mL/min/1.73 m(2). Lumbar spine bone mineral density (BMD), bone turnover markers (BTMs) and adverse events were evaluated at 48 weeks. RESULTS: Adverse event incidence was similar among three subgroups. There was also no exacerbation of impaired kidney function associated with Risedronate administration in the subjects with eGFR above 30 mL/min/1.73 m(2). Risedronate administration induced a significant increase in lumbar spine BMD and significant inhibition of BTMs in three subgroups. CONCLUSIONS: The Risedronate therapy showed similar clinical effects in CKD patients with osteoporosis compared to those without CKD.

Effect of Sequential Treatment with Bisphosphonates After Teriparatide in Ovariectomized Rats: A Direct Comparison Between Risedronate and Alendronate.[Pubmed:28337514]

Calcif Tissue Int. 2017 Jul;101(1):102-110.

Teriparatide (TPTD), a recombinant human parathyroid hormone N-terminal fragment (1-34), is a widely used bone anabolic drug for osteoporosis. Sequential treatment with antiresorptives such as bisphosphonates after TPTD discontinuation is generally recommended. However, relative effects of bisphosphonates have not been determined. In the present study, we directly compared effects of Risedronate (RIS) and alendronate (ALN) on bone mineral density (BMD), bone turnover, structural property and strength in ovariectomized (OVX) rats, when administered after TPTD. Female Sprague Dawley rats were divided into one sham-operated and eight ovariectomized groups. TPTD, RIS, and ALN were given subcutaneously twice per week for 4 or 8 weeks after 4 week treatment with TPTD. TPTD significantly increased BMD (+9.6%) in OVX rats after 4 weeks of treatment. 8 weeks after TPTD withdrawal, vehicle-treated group showed a blunted BMD increase of +8.4% from the baseline. In contrast, 8 weeks of treatment with RIS and ALN significantly increased BMD to 17.4 and 21.8%, respectively. While ALN caused a consistently larger increase in BMD, sequential treatment with RIS resulted in lower Tb.Sp compared to ALN in the fourth lumbar vertebra as well as in greater stiffness in compression test. In conclusion, the present study demonstrated that sequential therapy with ALN and RIS after TPTD both improved bone mass and structure. Our results further suggest that RIS may have a greater effect on improving bone quality and stiffness than ALN despite less prominent effect on BMD. Further studies are necessary to determine clinical relevance of these findings to fracture rate.

Description

Risedronic acid (Risedronate ) is a pyridinyl biphosphonate which inhibits osteoclast-mediated bone resorption.

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