NifedipineA selective calcium channel protein inhibitor

Nifedipine (CAS 21829-25-4)

Nifedipine | CAS 21829-25-4 is rated 5.0 out of 5 by 1.
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Synonym: Procardia; L-Type Calcium Channel Blocker III
Application: A selective calcium channel protein inhibitor
CAS Number: 21829-25-4
Purity: ≥98%
Molecular Weight: 346.33
Molecular Formula: C17H18N2O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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Nifedipine is a selective hypertensive calcium channel protein inhibitor which targets L-type voltage-sensitive calcium channels. Nifedipine is a vasodilator that is selective for inotropic over chronotropic cardiac effects. It has also been shown to induce apoptosis in human glioblastoma cells and inhibit advanced glycation end product-induced mesangial cell damage in vitro. Additionally, nifedipine has been suggested to work as an antioxidant and antiinflammatory agent against AGEs in tubular cells by suppressing RAGE expression via PPAR-γ activation.


References

1. Godfraind, T., et al. 1986. Pharmacol. Rev. 38: 321-416. PMID: 2432624
2. Miller, R.J., 1987. Science. 235: 46-52. PMID: 2432656
3. Segawa, D., et al. 1999. Eur. J. Pharmacol. 380: 123-128. PMID: 10513571
4. Zangar, R.C., et al. 1999. J. Pharmacol. Exp. Ther. 290: 1436-1441. PMID: 10454523
5. Eliot, L.A. and Jamali, F. 1999. J. Pharmacol. Exp. Ther. 291: 188-193. PMID: 10490903
6. Matsui, T., et al. 2010. Biochem. Biophys. Res. Commun. 398: 326-330. PMID: 20599709

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mg/ml), acetone (250 g/L) at 20° C, dichloromethane (160 g/L) at 20° C, chloroform (140 g/L) at 20° C, ethyl acetate (50 g/L) at 20° C, methanol (26 g/L) at 20° C, ethanol (17 g/L) at 20° C, buffer solutions of pH4 (0.0058 g/L) at 37° C, buffer solutions of pH7 (0.0056 g/L) at 37° C, buffer solutions of pH9.0 (0.0078 g/L) at 37° C, and buffer solutions of pH13 (0.006 g/L) at 37° C. Insoluble in water.
Storage :
Store at room temperature
Melting Point :
173-177° C
Refractive Index :
n20D 1.56
IC50 :
Voltage-gated L-type calcium channel alpha-1C subunit: IC50 = 1 nM (Oryctolagus cuniculus); Rattus norvegicus: IC50 = 1.16 nM (Rattus norvegicus); Oryctolagus cuniculus: IC50 = 0.5 nM (Oryctolagus cuniculus); Voltage-gated L-type calcium channel alpha-1D subunit: IC50 = 2.5 nM (human); Aorta: IC50 = 9 nM (Cavia porcellus); Sus scrofa: IC50 = 3.6 nM (Sus scrofa); Cavia porcellus: IC50 = 4 nM (Cavia porcellus); Voltage-gated L-type calcium channel alpha-1C subuni: IC50 = 2.53 nM (Rattus norvegicus); Rattus norvegicus: EC5050 = 3.2 nM (Rattus norvegicus); Transient receptor potential cation channel subfamily A member 1: EC5050 = 400 nM (Mus musculus)
Ki Data :
Voltage-gated L-type calcium channel alpha-1C subunit: Ki= 3.5 nM (Rattus norvegicus); Voltage-gated P/Q-type calcium channel alpha-1A subunit: Ki= 0.53 nM (Rattus norvegicus); Voltage-gated L-type calcium channel alpha-1D subunit: Ki= 1.2 nM (Rattus norvegicus); Voltage-gated L-type calcium channel alpha-1C subunit: Ki= 1 nM (human)
pK Values :
pKb: 2.69
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
1
RTECS :
US7975000
PubChem CID :
4485
Merck Index :
14: 6528
MDL Number :
MFCD00057326
EC Number :
244-598-3
Beilstein Registry :
497773
SMILES :
CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC

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Nifedipine  Product Citations

See how others have used Nifedipine. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 12 total

PMID: # 28065690  Semenova, G. et al. 2017. Biochimie. 135: 1-5.

PMID: # 16319189  Yamaguchi, T. et al. 2006. J. Am. Soc. Nephrol. 17: 178-187.

PMID: # 15952036  Szabó, G. et al. 2005. Pflugers Arch. 450: 307-316.

PMID: # 14871879  Lasaitiene, D. et al. 2004. Am J Physiol Renal Physiol. 286: F1144-F1153.

PMID: # 11790716  Shizukuda, Y. et al. 2002. Circulation. 105: -.

PMID: # 11435416  Morimoto, T. et al. 2001. J. Biol. Chem. 276: 34983-34989.

PMID: # 10948089  Fisslthaler, B. et al. 2000. Hypertension. 36: 270-275.

PMID: # 10646870  Miyake, H. et al. 2000. Cancer Res. 60: 170-176.

PMID: # 11120701  Matsunaga, T. et al. 2000. Circulation. 102: 3098-3103.

PMID: # 10400674  Miller, B.A. et al. 1999. J. Biol. Chem. 274: 20465-20472.

Citations 1 to 10 of 12 total
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Rated 5 out of 5 by from Yamaguchi Yamaguchi, et. al. (PubMed ID 16319189) used a calcium channel blocker, nifedipine in the course of their study regarding restoration of normal proliferation phenotype in human polycystic kidney disease epithelial cells. -SCBT Publication Review
Date published: 2015-03-10
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