| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
(Rac)-Upacicalcet targets the calcium-sensing receptor (CaSR), a G protein-coupled receptor that senses extracellular calcium levels and regulates parathyroid hormone (PTH) secretion. By activating CaSR, calcimimetics reduce PTH secretion, thereby lowering serum calcium and phosphate levels. This mechanism is used in the treatment of secondary hyperparathyroidism in patients with chronic kidney disease and primary hyperparathyroidism.
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|---|---|
| ln Vitro |
In vitro, (Rac)-Upacicalcet is a calcimimetic that activates the calcium-sensing receptor. It modulates CaSR signaling and reduces PTH secretion in parathyroid cells. However, specific IC50 values and detailed in vitro activity data are not extensively reported in the available literature. The compound is used as a research tool for studying calcium homeostasis and parathyroid function.
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| ln Vivo |
In vivo, (Rac)-Upacicalcet is expected to show efficacy in animal models of hyperparathyroidism by activating CaSR and reducing PTH secretion. However, specific in vivo efficacy data and dosing regimens are not extensively reported in the available literature. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (Rac)-Upacicalcet typically involve CaSR activation assays using cells expressing the calcium-sensing receptor. Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4) and treated with various concentrations of the compound (0.001-100 μM). Intracellular calcium mobilization is measured by fluorescence. The EC50 for CaSR activation is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for (Rac)-Upacicalcet use parathyroid cells or cell lines expressing CaSR. Cells are cultured in appropriate media and treated with various concentrations of the compound (0.001-10 μM) for 1-24 hours. PTH secretion is measured by ELISA. Intracellular calcium levels are measured using fluorescent indicators. Cell viability is assessed using MTT assays.
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| Animal Protocol |
In vivo animal studies with (Rac)-Upacicalcet would typically use rodent models of hyperparathyroidism. The compound would be administered orally or intraperitoneally at doses of 1-30 mg/kg. Serum calcium, phosphate, and PTH levels would be measured. However, specific protocols are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Rac)-Upacicalcet are not extensively reported. As a calcimimetic, it is expected to have oral bioavailability. Specific PK parameters such as half-life, volume of distribution, and clearance are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of (Rac)-Upacicalcet is not extensively reported. As a calcimimetic, potential toxicities may include hypocalcemia and gastrointestinal effects. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
(Rac)-Upacicalcet (CAS 2649575-19-7) is a racemic mixture of Upacicalcet, a calcimimetic agent that targets the calcium-sensing receptor (CaSR). It is used in research on mineral metabolism and parathyroid disorders. However, specific IC50 values and detailed activity data are not extensively reported. The compound is available for research purposes only.
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| Molecular Formula |
C11H14CLN3O6S
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|---|---|
| Molecular Weight |
351.76
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| Exact Mass |
351.029
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| CAS # |
2649575-19-7
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| Related CAS # |
Upacicalcet sodium;2052969-18-1;Upacicalcet;1333218-50-0
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| PubChem CID |
76026235
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| Appearance |
White to off-white solid powder
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| LogP |
-2.9
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
522
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C(O)=O)(N)CNC(=O)NC1=CC(=CC(Cl)=C1C)S(O)(=O)=O
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| InChi Key |
LHEYGVSDVBEYQF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H14ClN3O6S/c1-5-7(12)2-6(22(19,20)21)3-9(5)15-11(18)14-4-8(13)10(16)17/h2-3,8H,4,13H2,1H3,(H,16,17)(H2,14,15,18)(H,19,20,21)
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| Chemical Name |
2-amino-3-[(3-chloro-2-methyl-5-sulfophenyl)carbamoylamino]propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~284.28 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8428 mL | 14.2142 mL | 28.4285 mL | |
| 5 mM | 0.5686 mL | 2.8428 mL | 5.6857 mL | |
| 10 mM | 0.2843 mL | 1.4214 mL | 2.8428 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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