2. GPCR/G Protein
  3. CaSR
  4. Upacicalcet

Upacicalcet  (Synonyms: SK-1403 free acid; AJT240 free acid; PLS240 free acid)

Cat. No.: HY-109106
Handling Instructions Technical Support

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Upacicalcet sodium) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Upacicalcet

Upacicalcet Chemical Structure

CAS No. : 1333218-50-0

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Upacicalcet Related Antibodies

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Description

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[1][2].

IC50 & Target

calcium-sensing receptors[1]
In Vitro

Upacicalcet (0.0001-10 μM) sodium increases the intracellular Ca2+ and IP-1 (EC50 = 26.1 nM) in the presence of 1.2mM Ca2+ in human CaSR-expressing HEK293T (CaSR-HEK) cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Upacicalcet Related Antibodies
In Vivo

Upacicalcet (0.3-30 mg/kg, i.v.; s.c., once) sodium reduces serum iPTH, Ca2+, and Pi levels, does not affect gastric emptying in male SD rats and double-nephrectomized SD rats[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.

Animal Model: Male SD rats[1]
Dosage: 0.03 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: i.v.; s.c., once
Result: Reduced serum iPTH, Ca2+, and Pi levels.
Did not affect gastric emptying.
Animal Model: Double-nephrectomized SD rats[1]
Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg
Administration: i.v., once
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.
Animal Model: Adenine- induced (0.75 % Adenine in CE-2 solid diet) CKD Male SD rats (twelve-week-old) model[2]
Dosage: 0.2 mg/kg, 1 mg/kg
Administration: i.v., three times a week for 3 weeks
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.
Animal Model: Adenine-induced (0.75 % Adenine in CE-2 solid diet) renal failure male Wistar rats (nine-week-old) model[2]
Dosage: 1 mg/kg
Administration: s.c., once a day, 28 days
Result: Suppressed serum iPTH levels.
Inhibited the cortical porosity of the right femur and the volume of fibrosis in the right tibia.
Molecular Weight

351.76

Formula

C11H14ClN3O6S
CAS No.
SMILES

O=C(NC[C@H](N)C(O)=O)NC1=CC(S(=O)(O)=O)=CC(Cl)=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Upacicalcet Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Upacicalcet1333218-50-0SK-1403AJT240PLS240SK1403SK 1403AJT 240AJT-240PLS 240PLS-240CaSRCalcium-sensing receptorcalcium-sensing receptorscalcimimetic agentparathyroid hormonePTHsecondary hyperparathyroidismSHPTCaSR-HEK cellsCKDInhibitorinhibitorinhibit

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