NPS-2143


Catalog No. Size PriceQuantity
M7846-2 2mg solid $100
M7846-10 10mg solid $300

Description

NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.

Product information

CAS Number: 284035-33-2

Molecular Weight: 408.92

Formula: C24H25ClN2O2

Synonym:

SB-262470A

Related CAS Number:

324523-20-8 (NPS-2143 hydrochloride)

Chemical Name: 2-chloro-6-[(2R)-2-hydroxy-3-{[2-methyl-1-(naphthalen-2-yl)propan-2-yl]amino}propoxy]benzonitrile

Smiles: CC(C)(CC1C=C2C=CC=CC2=CC=1)NC[C@@H](O)COC1=CC=CC(Cl)=C1C#N

InChiKey: PZUJQWHTIRWCID-HXUWFJFHSA-N

InChi: InChI=1S/C24H25ClN2O2/c1-24(2,13-17-10-11-18-6-3-4-7-19(18)12-17)27-15-20(28)16-29-23-9-5-8-22(25)21(23)14-26/h3-12,20,27-28H,13,15-16H2,1-2H3/t20-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 82 mg/mL (200.53 mM) Water Insoluble

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:

NPS 2143 blocks increases in cytoplasmic Ca2+ concentrations with IC50 of 43 nM elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. NPS 2143 stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation. In HEK-293 cells transiently expressing hCaSRs, NPS 2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH (data not shown) and γ-Glu-Val-Gly. A recent study shows that NPS 2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells.

In Vivo:

In rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels. In normotensive rats, NPS 2143 administration (1 mg/kg) by i.v. markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands.

References:

  1. Nemeth EF, et al. J Pharmacol Exp Ther. 2001, 299(1), 323-331.
  2. Rybczynska A, et al. J Endocrinol. 2006, 191(1), 189-195.
  3. Ohsu T, et al. J Biol Chem. 2010, 285(2), 1016-1022.
  4. Nakajima S, et al. Mol Nutr Food Res. 2012, 56(5), 753-760.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed