A-75943
A-75943 is a bone resorption inhibitor isolated from Streptomyces sp. SANK 61296, with protein synthesis toxicity. A-75943 inhibits bone resorption in vitro, and also suppresses the increase in serum calcium levels and the decrease in bone mineral density in thyroparathyroidectomized rats. A-75943 inhibits protein synthesis. High concentrations of A-75943 reduce the survival rate of osteoclasts on bone slices, while low concentrations have no effect on the survival rate or morphology of osteoclasts. A-75943 can be used for the research of osteoporosis and hypercalcemia.
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- CAS No.: 201215-10-3
- 화학식: C15H23NO4
- 분자량:281.35
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
A-75943 (3-30 mg/kg; s.c.; daily; day 4 to day 10 post-thyroparathyroidectomy) dose-dependently suppresses Ro13-6298 (HY-106735)-induced increases in serum Ca2+ and decreases in bone mineral density in thyroparathyroidectomized rats, with the 30 mg/kg dose producing the strongest effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar Imamichi (male, 8-week-old, thyroparathyroidectomized)[1]
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Dosage:3 mg/kg; 30 mg/kg
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Administration:s.c.; daily; day 4 to day 10 post-thyroparathyroidectomy
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Result:Suppressed Ro-136298-induced increases in serum Ca2+ and decreases in bone mineral density in a dose-dependent manner.
Achieved serum Ca2+ concentrations of 6.99 mg/dl on day 0, 10.66 mg/dl on day 5, and 12.51 mg/dl on day 7 at 3 mg/kg.
Reached bone mineral density of 129.9 mg/cm2 at 3 mg/kg.
Achieved serum Ca2+ concentrations of 6.92 mg/dl on day 0, 8.14 mg/dl on day 5, and 9.29 mg/dl on day 7 at 30 mg/kg.
Reached bone mineral density of 134.4 mg/cm2 at 30 mg/kg.
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Animal Model:Wistar Imamichi (male, 8-week-old, thyroparathyroidectomized)[1]
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Dosage:10 mg/kg
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Administration:s.c.; daily; day 4 to day 10 post-thyroparathyroidectomy
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Result:Suppressed Ro-136298-induced increases in serum Ca2+ and decreases in bone mineral density.
Achieved serum Ca2+ concentrations of 5.71 mg/dl on day 0, 8.85 mg/dl on day 5, and 12.04 mg/dl on day 7.
Reached bone mineral density of 128.3 mg/cm2.
Chemical Information
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CAS No. 201215-10-3
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분자량 281.35
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화학식 C15H23NO4
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SMILES
O=C1[C@]([C@]2(C[C@@H](CC(N)=O)CC(=O)O2)[H])(C[C@@H](C)C[C@@H]1C)[H]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- A-75943
- 201215-10-3
- A75943
- A 75943
- Antibiotic
- Endogenous Metabolite
- Streptomyces sp. SANK 61296
- protein synthesis
- osteoporosis
- hypercalcemic diseases
- thyroid and parathyroid-extracted rats
- osteoclast
- bone mineral density
- thyroparathyroidectomized rats
- bone resorption
- mouse unfractionated bone cell cultures
- Inhibitor
- inhibitor
- inhibit