NPS-2143
Catalog No.: GC16943Purity:>99.00%
NPS-2143 (SB-262470A) ، عامل مكلس نشط عن طريق الفم ، هو مضاد انتقائي وفعال لمستقبلات استشعار أيون الكالسيوم (CaSR)
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
Cas No.: 284035-33-2
10mM (in 1mL DMSO)In Stock
$53.00
1
1mgIn Stock
$15.00
1
5mgIn Stock
$45.00
1
10mgIn Stock
$59.00
1
25mgIn Stock
$130.00
1
50mgIn Stock
$221.00
1
100mgIn Stock
$405.00
1
200mgIn Stock
$675.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $53.00 | In Stock | 1 | |
| 1mg | $15.00 | In Stock | 1 | |
| 5mg | $45.00 | In Stock | 1 | |
| 10mg | $59.00 | In Stock | 1 | |
| 25mg | $130.00 | In Stock | 1 | |
| 50mg | $221.00 | In Stock | 1 | |
| 100mg | $405.00 | In Stock | 1 | |
| 200mg | $675.00 | In Stock | 1 |
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المراجع (Citations)
3 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
NPS-2143 is an orally active calcium-sensing receptor (CaSR) antagonist that induces an increase in cytosolic Ca2+ concentration, with an IC50 of 43nM. NPS-2143 stimulates the release of parathyroid hormone[1].
NPS-2143 (100nM; 30min) effectively inhibits the secretion of cytokines and chemokines induced by fAβ25–35 in NHA cell, including IL-6, MCP-2, RANTES, and s-ICAM-1[2]. NPS-2143 significantly inhibits cell proliferation in MDA-MB-231 and MCF-7 cells, with IC50 values of 4.08μM and 5.71μM, respectively. In MDA-MB-231 cells, NPS-2143 induces caspase-3/7 activation while significantly reducing the expression of the anti-apoptotic protein Bcl-2. Additionally, NPS-2143 inhibits the migration and invasion of MDA-MB-231 cells and significantly downregulates the expression of p-ERK1/2 and integrin β1 proteins[3].
NPS-2143 (30mg/kg) was administered as a single intraperitoneal injection to wild-type and Nuf mice, plasma calcium and PTH concentrations, as well as urinary calcium excretion were measured. NPS-2143 caused a significant increase in plasma calcium and PTH levels in Nuf mice but did not increase urinary calcium excretion. NPS-2143 normalized the gain-of-function mutation causing ADH1 and ameliorated the hypocalcemia associated with the disease[4].
References:
[1].Wang S, Qiu L, et al. NPS - 2143 (hydrochloride) inhibits melanoma cancer cell proliferation and induces autophagy and apoptosis. Med Sci (Paris). 2018 Oct;34 Focus issue F1:87-93.
[2].Chiarini A, Armato U, et al. CaSR Antagonist (Calcilytic) NPS 2143 Hinders the Release of Neuroinflammatory IL-6, Soluble ICAM-1, RANTES, and MCP-2 from Aβ-Exposed Human Cortical Astrocytes. Cells. 2020 Jun 2;9(6):1386.
[3].Alqudah MAY, Azaizeh M, et al. Calcium-Sensing Receptor Antagonist NPS-2143 Inhibits Breast Cancer cell Proliferation, Migration and Invasion via Downregulation of p-ERK1/2, Bcl-2 and Integrin β1 and Induces Caspase 3/7 Activation. Adv Pharm Bull. 2022 Mar;12(2):383-388.
[4].Hannan FM, Walls GV, et al. The Calcilytic Agent NPS 2143 Rectifies Hypocalcemia in a Mouse Model With an Activating Calcium-Sensing Receptor (CaSR) Mutation: Relevance to Autosomal Dominant Hypocalcemia Type 1 (ADH1). Endocrinology. 2015 Sep;156(9):3114-21.
البروتوكول (Protocol)
| Cell experiment [1]: | |
|
Cell lines |
Breast cancer cell lines MDA-MB-231 and MCF-7 |
|
Preparation Method |
The biological effects of various concentrations of NPS-2143 on breast cancer cell proliferation were measured by in vitro MTT assay. |
|
Reaction Conditions |
0.5-10µM; 48h |
|
Applications |
The cell viability of both MDA-MB-231 and MCF-7 cells was reduced after NPS-2143 treatment in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Wild-type, Nuf/+, and Nuf/Nuf mice |
|
Preparation Method |
A single bolus of NPS-2143 or vehicle (15% aqueous solution of 2-hydroxypropyl- β-cyclodextrin) was administered to mice. Plasma samples were obtained at either 0, 1, 4, or 24 hours by tail vein or terminal bleed. |
|
Dosage form |
30mg/kg; once; i.p. |
|
Applications |
NPS-2143 successfully improved the hypocalcemia associated with Nuf/+ and Nuf/Nuf mice compared with mice given the drug vehicle alone or untreated mice. At 4 hours after NPS 2143 administration, plasma calcium values remained significantly elevated in wild-type and affected Nuf/+ mice compared with respective untreated mice. |
References: [1]. Alqudah MAY, Azaizeh M, et al. Calcium-Sensing Receptor Antagonist NPS-2143 Inhibits Breast Cancer cell Proliferation, Migration and Invasion via Downregulation of p-ERK1/2, Bcl-2 and Integrin β1 and Induces Caspase 3/7 Activation. Adv Pharm Bull. 2022 Mar;12(2):383-388. [2]. Hannan FM, Walls GV, et al. The Calcilytic Agent NPS 2143 Rectifies Hypocalcemia in a Mouse Model With an Activating Calcium-Sensing Receptor (CaSR) Mutation: Relevance to Autosomal Dominant Hypocalcemia Type 1 (ADH1). Endocrinology. 2015 Sep;156(9):3114-21. | |
وثائق المنتج (Product Documents)
Purity:>99.00%Appearance:A solid
البيانات البيولوجية (Biological Data)
1 / 1
الخصائص الكيميائية (Chemical Properties)
رقم CAS
284035-33-2
الاسم الكيميائي
2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
SMILES
CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O
الصيغة الجزيئية
C24H25ClN2O2
الوزن الجزيئي
408.93
الذوبانية
≥ 40.9mg/mL in DMSO
التخزين
Store at -20°C
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
g/mol
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