NPS-2143 hydrochloride
Based on 30 publication(s) in Google Scholar
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.
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- Pureza : 99.98%
- No. CAS: 324523-20-8
- Fòrmula: C24H26Cl2N2O2
- Peso molecular:445.38
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NPS-2143 hydrochloride
More- Int J Biol Sci. 2024 Jul 15;20(10):3892-3910. [Abstract]
- Phytomedicine. 2021 Apr:84:153507. [Abstract]
- Food Chem. 2025 Feb 1;464(Pt 1):141569. [Abstract]
- Int J Mol Med. 2021 Jan;47(1):302-314. [Abstract]
- J Agric Food Chem. 2025 Apr 25. [Abstract]
- Food Funct. 2025 Mar 26. [Abstract]
- Food Funct. 2022 Jun 6;13(11):6233-6243. [Abstract]
- Acta Physiol. 2026 Jan;242(1):e70142. [Abstract]
- Acta Physiol. 2023 Apr;237(4):e13926. [Abstract]
- Int J Mol Sci. 2023 Mar 3;24(5):4921. [Abstract]
- J Clin Endocrinol Metab. 2025 Jun 17;110(7):1865-1880. [Abstract]
- Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]
- Bioorg Chem. 2026 Feb:169:109418. [Abstract]
- Sci Rep. 2025 May 9;15(1):16209. [Abstract]
- Sci Rep. 2019 Dec 12;9(1):18979. [Abstract]
- J Food Sci. 2018 Sep;83(9):2394-2401. [Abstract]
- J Tradit Complement Med. 2024 Jul 2;15(5):495-508. [Abstract]
- Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. [Abstract]
- PeerJ. 2026 Jan 5:14:e20546. [Abstract]
- Toxicon. 2026 Jan:269:108660. [Abstract]
- FEBS Open Bio. 2025 Oct 13. [Abstract]
- Photochem Photobiol. 2022 Sep;98(5):1157-1166. [Abstract]
- FASEB Bioadv. 2025 Sep 3;7(8):e70045. [Abstract]
- Neurosci Lett. 2025 Oct 14:865:138351. [Abstract]
- Gen Comp Endocrinol. 2018 Oct 1:267:1-8. [Abstract]
- J Vet Sci. 2018 Mar 31;19(2):179-187. [Abstract]
- University of Verona. 2025.
- University of Verona. 2025.
- Oxid Med Cell Longev. 2021 Jan 12:2021:3010548. [Abstract]
- Oxid Med Cell Longev. 2017:2017:3869561. [Abstract]
Customer Validation & Images
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.003 μM
Compound: 38, (NPS 2143,SB-262470A)
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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
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[PMID: 19492813] |
| HEK293 | IC50 |
0.043 μM
Compound: 38, (NPS 2143,SB-262470A)
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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
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[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 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.
Chemical Information
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No. CAS 324523-20-8
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Appearance Solid
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Peso molecular 445.38
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Fòrmula C24H26Cl2N2O2
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Color White to off-white
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SMILES
N#CC1=C(OC[C@@H](CNC(C)(C)CC2=CC=C3C=CC=CC3=C2)O)C=CC=C1Cl.[H]Cl
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Synonyms
SB-262470A hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (30)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
The Interaction of Calcium-Sensing Receptor with KIF11 Enhances Cisplatin Resistance in Lung Adenocarcinoma via BRCA1/cyclin B1 pathway. [Abstract]2024 Jul 15;20(10):3892-3910. PMID: 39113697 -
Phytomedicine
Matrine, as a CaSR agonist promotes intestinal GLP-1 secretion and improves insulin resistance in diabetes mellitus. [Abstract]2021 Apr:84:153507. PMID: 33636577 -
Food Chem
Targeted discovery of pea protein-derived GLP-1-secreting peptides by CaSR activation-based molecular docking and their digestive stability. [Abstract]2025 Feb 1;464(Pt 1):141569. PMID: 39418954 -
Int J Mol Med
Astragaloside IV attenuates cerebral ischemia‑reperfusion injury in rats through the inhibition of calcium‑sensing receptor‑mediated apoptosis. [Abstract]2021 Jan;47(1):302-314. PMID: 33416112 -
J Agric Food Chem
Novel Cholecystokinin Secretion-Stimulating Peptides from Oat Protein Hydrolysate: Sequence Identification and Insight into the Mechanism of Action. [Abstract]2025 Apr 25. PMID: 40275796 -
Food Funct
Bioactive peptides from barley protein hydrolysate stimulate cholecystokinin secretion via calcium-sensing receptor signaling in enteroendocrine cells. [Abstract]2025 Mar 26. PMID: 40134323 -
Food Funct
Digestion characteristics of quinoa, barley and mungbean proteins and the effects of their simulated gastrointestinal digests on CCK secretion in enteroendocrine STC-1 cells. [Abstract]2022 Jun 6;13(11):6233-6243. PMID: 35587126 -
Acta Physiol
Upregulated Calcium Sensing Receptor Mediates Pulmonary Venous Remodeling in Pulmonary Hypertension. [Abstract]2026 Jan;242(1):e70142. PMID: 41387174 -
Acta Physiol
2023 Apr;237(4):e13926. PMID: 36606511 -
Int J Mol Sci
The CaSR Modulator NPS-2143 Reduced UV-Induced DNA Damage in Skh:hr1 Hairless Mice but Minimally Inhibited Skin Tumours. [Abstract]2023 Mar 3;24(5):4921. PMID: 36902353 -
J Clin Endocrinol Metab
Heterogenous Origins of Calcium Homeostasis Disorders Arising from Five Heterozygous Calcium-Sensing Receptor Variants. [Abstract]2025 Jun 17;110(7):1865-1880. PMID: 39413244 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Bioorg Chem
L-tetrahydropalmatine attenuates methamphetamine-induced pulmonary vascular remodeling via CaSR-BMP2/mTOR signaling. [Abstract]2026 Feb:169:109418. PMID: 41443015 -
Sci Rep
NPS-2143 suppresses malignant phenotypes of retinoblastoma cells involved in regulating NF-κB pathway. [Abstract]2025 May 9;15(1):16209. PMID: 40346093 -
Sci Rep
Shape-dependent toxicity and mineralization of hydroxyapatite nanoparticles in A7R5 aortic smooth muscle cells. [Abstract]2019 Dec 12;9(1):18979. PMID: 31831831 -
J Food Sci
Sensing of L-Arginine by Gut-Expressed Calcium Sensing Receptor Stimulates Gut Satiety Hormones Cholecystokinin and Glucose-Dependent Insulinotropic Peptide Secretion in Pig Model. [Abstract]2018 Sep;83(9):2394-2401. PMID: 30088839 -
J Tradit Complement Med
Xinbao pill attenuated water retention by regulating the CaSR/AQP2 pathway in LAD-induced chronic heart failure rats. [Abstract]2024 Jul 2;15(5):495-508. PMID: 40979484 -
Am J Physiol Heart Circ Physiol
Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart. [Abstract]2010 Nov;299(5):H1309-17. PMID: 20833954
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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PeerJ
Cholesterol and steroid synthesis pathways may be involved in the inhibition of osteosarcoma cell viability by calcium-sensing receptor antagonism. [Abstract]2026 Jan 5:14:e20546. PMID: 41522513 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198 -
FEBS Open Bio
Calcium-sensing receptor induces the apoptosis of chondrocytes in cooperation with phosphate transporter. [Abstract]2025 Oct 13. PMID: 41081312 -
Photochem Photobiol
2022 Sep;98(5):1157-1166. PMID: 35288938 -
FASEB Bioadv
2025 Sep 3;7(8):e70045. PMID: 40909871 -
Neurosci Lett
Inhibition of calcium-sensing receptor by its antagonist protects dopaminergic neurons from MPTP/MPP+-induced neurotoxicity via regulating mitochondrial function, autophagy, and apoptosis in vivo and in vitro. [Abstract]2025 Oct 14:865:138351. PMID: 40789434 -
Gen Comp Endocrinol
Phenylalanine and tryptophan stimulate gastrin and somatostatin secretion and H+-K+-ATPase activity in pigs through calcium-sensing receptor. [Abstract]2018 Oct 1:267:1-8. PMID: 29782837 -
J Vet Sci
Calcium-sensing receptor-mediated L-tryptophan-induced secretion of cholecystokinin and glucose-dependent insulinotropic peptide in swine duodenum. [Abstract]2018 Mar 31;19(2):179-187. PMID: 29284209
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.
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Oxid Med Cell Longev
2021 Jan 12:2021:3010548. PMID: 33505580 -
Oxid Med Cell Longev
Expression and Role of the Calcium-Sensing Receptor in Rat Peripheral Blood Polymorphonuclear Neutrophils. [Abstract]2017:2017:3869561. PMID: 29081886
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.
Solvente y solubilidad
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.
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.
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.
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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
HY-10171 Related Classifications
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