Upacicalcet sodium
Based on 1 Customer Validation
Upacicalcet sodium is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet sodium reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet sodium sodium improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet sodium sodium inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet sodium is useful for studying SHPT.
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- Purity: 99.91%
- CAS No.: 2052969-18-1
- 화학식: C11H13ClN3NaO6S
- 분자량:373.75
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
calcium-sensing receptors[1]
Upacicalcet (0.2-1 mg/kg, i.v., three times a week for 3 weeks) sodium reduces serum iPTH levels and inhibits parathyroid hyperplasia in Adenine- induced CKD SD rats model[2].
Upacicalcet (1 mg/kg, s.c., once a day, 28 days) sodium reduces serum iPTH levels and inhibits ectopic calcification and cortical hole formation in Adenine- induced CKD Wistar rats model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rats[1]
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Dosage:0.03 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:i.v.; s.c., once
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Result:Reduced serum iPTH, Ca2+, and Pi levels.
Did not affect gastric emptying.
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Animal Model:Double-nephrectomized SD rats[1]
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Dosage:0.3 mg/kg, 3 mg/kg, 30 mg/kg
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Administration:i.v., once
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Result:Reduced serum iPTH, Ca2+ levels, lowered Ca2+ to a maximum of 8.2 mg/dL 24 hours after administration of 3 mg/kg or higher.
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Animal Model:Adenine- induced (0.75 % Adenine in CE-2 solid diet) CKD Male SD rats (twelve-week-old) model[2]
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Dosage:0.2 mg/kg, 1 mg/kg
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Administration:i.v., three times a week for 3 weeks
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Result:Suppressed serum iPTH levels, increased phosphorus, creatinine and urea nitrogen levels.
Reduced parathyroid gland size by 44% and 57%, respectively, and decreased Ki-67 positive cell density compared to CKD controls.
Reduced Ca2+ content and von Kossa-positive area in the thoracic aorta.
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Animal Model:Adenine-induced (0.75 % Adenine in CE-2 solid diet) renal failure male Wistar rats (nine-week-old) model[2]
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Dosage:1 mg/kg
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Administration:s.c., once a day, 28 days
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Result:Suppressed serum iPTH levels.
Inhibited the cortical porosity of the right femur and the volume of fibrosis in the right tibia.
Chemical Information
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CAS No. 2052969-18-1
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Appearance Solid
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분자량 373.75
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화학식 C11H13ClN3NaO6S
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Color White to off-white
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SMILES
O=C(NC[C@H](N)C(O[Na])=O)NC1=CC(S(=O)(O)=O)=CC(Cl)=C1C
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Synonyms
SK-1403; AJT240; PLS240
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (267.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Goto M, et al. Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo. Eur J Pharmacol. 2023 Oct 5;956:175936. [Content Brief]
[2]. Sato H, et al. Upacicalcet, a positive allosteric modulator of the calcium-sensing receptor, prevents vascular calcification and bone disorder in a rat adenine-induced secondary hyperparathyroidism model. Bone. 2023 Feb;167:116613. [Content Brief]
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6756 mL | 13.3779 mL | 26.7559 mL | 66.8896 mL |
| 5 mM | 0.5351 mL | 2.6756 mL | 5.3512 mL | 13.3779 mL | |
| 10 mM | 0.2676 mL | 1.3378 mL | 2.6756 mL | 6.6890 mL | |
| 15 mM | 0.1784 mL | 0.8919 mL | 1.7837 mL | 4.4593 mL | |
| 20 mM | 0.1338 mL | 0.6689 mL | 1.3378 mL | 3.3445 mL | |
| 25 mM | 0.1070 mL | 0.5351 mL | 1.0702 mL | 2.6756 mL | |
| 30 mM | 0.0892 mL | 0.4459 mL | 0.8919 mL | 2.2297 mL | |
| 40 mM | 0.0669 mL | 0.3344 mL | 0.6689 mL | 1.6722 mL | |
| 50 mM | 0.0535 mL | 0.2676 mL | 0.5351 mL | 1.3378 mL | |
| 60 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 80 mM | 0.0334 mL | 0.1672 mL | 0.3344 mL | 0.8361 mL | |
| 100 mM | 0.0268 mL | 0.1338 mL | 0.2676 mL | 0.6689 mL |
Upacicalcet sodium Related Classifications
HY-109106A Related Classifications
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