NPS-2143 hydrochloride (Synonyms: SB-262470A hydrochloride)

Name: NPS-2143 hydrochloride
Brand: MedChemExpress
SKU: HY-10171
Rating: 5.0 (21 reviews)

Cat. No.: HY-10171 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

NPS-2143 hydrochloride Chemical Structure

CAS No. : 324523-20-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 114	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 114	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 49	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 104	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 431	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 21 publication(s) in Google Scholar

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NPS-2143 In-stock

18 Publications Citing Use of MCE NPS-2143 hydrochloride

: NPS-2143 hydrochloride purchased from MedChemExpress. Usage Cited in: J Vet Sci. 2018 Mar 31;19(2):179-187. [Abstract]; The protein levels of calcium-sensing receptor (CaSR) and its signal molecules regulated by CaSR antagonist NPS 2143. The protein images of CaSR, protein kinase C (PKC), and inositol trisphosphate receptor (IP3R) in the presence of 20 mM tryptophan and NPS 2143.

: NPS-2143 hydrochloride purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017;2017:3869561. [Abstract]; N-formyl-Met-Leu-Phe (fMLP; 10 nM) are used to stimulate the cells for 2 min, and the polymorphonuclear neutrophils (PMNs) without fMLP serve as the control. NPS-2143 (100 nM), Cinacalcet (100 nM), and PDTC (100 nM) are added and incubated. Protein expression results are representative of three experiments.

: NPS-2143 hydrochloride purchased from MedChemExpress. Usage Cited in: Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. [Abstract]; Distribution of cardioprotective signaling kinases among fractions prepared from perfusion, IPC, and NPS2143-treated IPC hearts. After nondetergent caveolae fractionation via sucrose gradient ultracentrifugation, equal volume of each collected sucrose fraction is subjected to 4–12% SDS-PAGE under reducing condition and followed with p-ERK1/2 (A), p-AKT (B), and p-GSK-3β (C) IB detection. The representative IBs are taken and shown from one out of three independent experiments.

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.003 μM Compound: 38, (NPS 2143,SB-262470A)	Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay	[PMID: 19492813]
HEK293	IC₅₀	0.043 μM Compound: 38, (NPS 2143,SB-262470A)	Antagonist activity at human calcium receptor 1 expressed in HEK293 4.0-7 cells assessed as inhibition of extracellular calcium-induced increase in intracellular calcium level by FLIPR assay Antagonist activity at human calcium receptor 1 expressed in HEK293 4.0-7 cells assessed as inhibition of extracellular calcium-induced increase in intracellular calcium level by FLIPR assay	[PMID: 19492813]

In Vitro

NPS-2143 hydrochloride (SB-262470A hydrochloride) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC₅₀ of 41 nM. Moreover, NPS-2143 hydrochloride 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

When infused intravenously in normal rats, NPS-2143 hydrochloride (SB-262470A hydrochloride) causes a rapid and large increase in plasma levels of PTH. Ca²⁺ receptor antagonists are termed calcilytics and NPS-2143 is the first substance (either atomic or molecular) shown to possess such activity^[1].
When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

445.38

Formula

C₂₄H₂₆Cl₂N₂O₂

CAS No.

324523-20-8

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(OC[C@@H](CNC(C)(C)CC2=CC=C3C=CC=CC3=C2)O)C=CC=C1Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°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 (224.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1.85 mg/mL (4.15 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2453 mL	11.2264 mL	22.4527 mL
5 mM	0.4491 mL	2.2453 mL	4.4905 mL
10 mM	0.2245 mL	1.1226 mL	2.2453 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (274 KB) SDS (537 KB)

COA (245 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

References

[1]. Huang Y, Breitwieser GE. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J Biol Chem. 2007 Mar 30;282(13):9517-25 [Content Brief]

[2]. Marquis, Robert W.; Lago, Amparo M.; Callahan, James F.;Antagonists of the Calcium Receptor. 2. Amino Alcohol-Based Parathyroid Hormone Secretagogues. Journal of Medicinal Chemistry (2009), 52(21), 6599-6605. [Content Brief]

[3]. Yamamura A, Guo Q, Yamamura H, Zimnicka AM, Pohl NM, Smith KA, Fernandez RA, Zeifman A, Makino A, Dong H, Yuan JX.Enhanced Ca2+-sensing receptor function in idiopathic pulmonary arterial hypertension.Circ Res. 2012 Aug 3;111(4):469-81. Epub 2012 Jun 22. [Content Brief]

[4]. Nakajima S, Hira T, Hara H.Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells.Mol Nutr Food Res. 2012 May;56(5):753-60. [Content Brief]

[5]. Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM, Christopoulos A.Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.Endocrinology. 2012 Mar;153(3):1232-41. Epub 2011 Dec 30. [Content Brief]

[6]. Nemeth EF, et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.2453 mL	11.2264 mL	22.4527 mL	56.1318 mL
DMSO	5 mM	0.4491 mL	2.2453 mL	4.4905 mL	11.2264 mL
	10 mM	0.2245 mL	1.1226 mL	2.2453 mL	5.6132 mL
	15 mM	0.1497 mL	0.7484 mL	1.4968 mL	3.7421 mL
	20 mM	0.1123 mL	0.5613 mL	1.1226 mL	2.8066 mL
	25 mM	0.0898 mL	0.4491 mL	0.8981 mL	2.2453 mL
	30 mM	0.0748 mL	0.3742 mL	0.7484 mL	1.8711 mL
	40 mM	0.0561 mL	0.2807 mL	0.5613 mL	1.4033 mL
	50 mM	0.0449 mL	0.2245 mL	0.4491 mL	1.1226 mL
	60 mM	0.0374 mL	0.1871 mL	0.3742 mL	0.9355 mL
	80 mM	0.0281 mL	0.1403 mL	0.2807 mL	0.7016 mL
	100 mM	0.0225 mL	0.1123 mL	0.2245 mL	0.5613 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

NPS-2143 hydrochloride Related Classifications

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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:

NPS-2143324523-20-8SB-262470ANPS2143NPS 2143CaSRCalcium-sensing receptorInhibitorinhibitorinhibit

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NPS-2143 hydrochloride (Synonyms: SB-262470A hydrochloride)

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Other Forms of NPS-2143 hydrochloride:

NPS-2143 hydrochloride Related Antibodies

18 Publications Citing Use of MCE NPS-2143 hydrochloride

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Purity & Documentation

References

Customer Review

NPS-2143 hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

NPS-2143 hydrochloride Related Classifications

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