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

Upacicalcet sodium  (Synonyms: SK-1403; AJT240; PLS240)

Cat. No.: HY-109106A Purity: 99.91%
COA
SDS
Handling Instructions Technical Support

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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Upacicalcet sodium

Upacicalcet sodium Chemical Structure

CAS No. : 2052969-18-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Upacicalcet sodium Related Antibodies

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Description

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[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 sodium 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

373.75

Formula

C11H13ClN3NaO6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6756 mL 13.3779 mL 26.7559 mL
5 mM 0.5351 mL 2.6756 mL 5.3512 mL
View the 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.91%

SDS (252 KB)

COA (248 KB) HNMR (154 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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
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Upacicalcet sodium Related Classifications

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:

Upacicalcet2052969-18-1SK-1403 AJT240 PLS240SK1403SK 1403AJT240AJT 240AJT-240PLS240PLS 240PLS-240CaSRCalcium-sensing receptorcalcium-sensing receptorscalcimimetic agentparathyroid hormonePTHsecondary hyperparathyroidismSHPTCaSR-HEK cellsCKDInhibitorinhibitorinhibit

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