1. GPCR/G Protein
  2. CaSR
  3. Tecalcet Hydrochloride

Tecalcet Hydrochloride (Synonyms: R-568 hydrochloride)

Cat. No.: HY-10167A Purity: 99.66%
Handling Instructions

Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+.

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

Tecalcet Hydrochloride Chemical Structure

Tecalcet Hydrochloride Chemical Structure

CAS No. : 177172-49-5

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+[1][2][3].

In Vitro

Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner[3].
Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca2+ to the left without affecting the maximal response and, thereby, decreases the EC50 value for extracellular Ca21 to 0.61±0.04 mM[3].

In Vivo

Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency[1].

Animal Model: 10-wk-old Male Sprague-Dawley rats weighing 310-350 g[1].
Dosage: 1.5 and 15 mg/kg.
Administration: Orally twice daily for 4 days.
Result: Did not significantly change serum 1,25 (OH)2D3 levels. In contrast, serum PTH levels were reduced by in a dose-dependent manner.
Clearly reduced the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg body wt), and by 50% at a high dose (15 mg/kg body wt), indicating an antiproliferative effect on PT cells.
Reduced PT cell volume in a dose-dependent manner.
Molecular Weight

340.29

Formula

C₁₈H₂₃Cl₂NO

CAS No.

177172-49-5

SMILES

C[[email protected]@H](NCCCC1=CC=CC=C1Cl)C2=CC=CC(OC)=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (146.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9387 mL 14.6933 mL 29.3867 mL
5 mM 0.5877 mL 2.9387 mL 5.8773 mL
10 mM 0.2939 mL 1.4693 mL 2.9387 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 99.66%

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Keywords:

TecalcetR-568R568R 568CaSRCalcium-sensing receptorInhibitorinhibitorinhibit

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Product Name:
Tecalcet Hydrochloride
Cat. No.:
HY-10167A
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