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+.
Product information
CAS Number: 177172-49-5
Molecular Weight: 340.29
Formula: C18H23Cl2NO
Synonym:
R-568 hydrochloride
Chemical Name: [3-(2-chlorophenyl)propyl][(1R)-1-(3-methoxyphenyl)ethyl]amine; chlorohydrogen
Smiles: Cl.COC1=CC(=CC=C1)[C@@H](C)NCCCC1=CC=CC=C1Cl
InChiKey: YJXUXANREVNZLH-PFEQFJNWSA-N
InChi: InChI=1S/C18H22ClNO.ClH/c1-14(16-8-5-10-17(13-16)21-2)20-12-6-9-15-7-3-4-11-18(15)19;/h3-5,7-8,10-11,13-14,20H,6,9,12H2,1-2H3;1H/t14-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (146.93 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner. 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.
In Vivo:
Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency.
References:
- Wada, M., et al. The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. Control of parathyroid cell growth via a calcium receptor. Journal of Clinical Investigation 100(12), 2977-2983 (1997).
- Nemeth, E.F., et al. The parathyroid calcium receptor: a novel therapeutic target for treating hyperparathyroidism. Pediatr.Nephrol. 10(3), 275-279 (1996).
- Nemeth, E.F., et al. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proceedings of the National Academy of Sciences of the United States of America 95(7), 4040-4045 (1998).
Products are for research use only. Not for human use.
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