Upacicalcet
Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT.
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- CAS No.: 1333218-50-0
- Formule: C11H14ClN3O6S
- Masse moléculaire:351.76
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1333218-50-0
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Masse moléculaire 351.76
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Formule C11H14ClN3O6S
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SMILES
O=C(NC[C@H](N)C(O)=O)NC1=CC(S(=O)(O)=O)=CC(Cl)=C1C
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Synonyms
SK-1403 free acid; AJT240 free acid; PLS240 free acid
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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