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.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
A-75943 (5 μg/mL; 2 days) inhibits bone resorption in mouse unfractionated bone cell cultures with an IC50 of 0.35 μM, achieving >90% inhibition at 5 μg/mL without cytotoxicity at lower concentrations[1].
A-75943 inhibits protein synthesis in vitro with an IC50 of 153 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
A-75943 (10 mg/kg; s.c.; daily; day 4 to day 10 post-thyroparathyroidectomy) suppresses Ro13-6298 (HY-106735)-induced increases in serum Ca2+ and decreases in bone mineral density in thyroparathyroidectomized rats[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)
A-75943 Related Classifications
HY-183495 Related Classifications
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- 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