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Chemical Structure| 72509-76-3 Chemical Structure| 72509-76-3

Structure of Felodipine
CAS No.: 72509-76-3

Chemical Structure| 72509-76-3

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Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker.

Synonyms: H 154/82; CGH-869; Felodipine, Agon, Felo-Puren, Felobeta, Felocor, Felodipin, Felodur Felogamma, Fensel, Flodil, Modip, Munobal, Perfudal, Plendil, Renedil

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Product Details of Felodipine

CAS No. :72509-76-3
Formula : C18H19Cl2NO4
M.W : 384.25
SMILES Code : O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OCC
Synonyms :
H 154/82; CGH-869; Felodipine, Agon, Felo-Puren, Felobeta, Felocor, Felodipin, Felodur Felogamma, Fensel, Flodil, Modip, Munobal, Perfudal, Plendil, Renedil
MDL No. :MFCD00868316
InChI Key :RZTAMFZIAATZDJ-UHFFFAOYSA-N
Pubchem ID :3333

Safety of Felodipine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302+H312+H332
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312+P330-P302+P352+P312+P362+P364-P304+P340+P312-P501

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

    L-type calcium channel, IC50:0.15 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
IPSC-derived human neurons 100 nM 5 days Felodipine reduced levels of A53T α-synuclein. Nat Commun. 2019 Apr 18;10(1):1817.
MRSE (ATCC 35984) 8 μg/mL 24 hours Evaluate the antibacterial effect of felodipine on MRSE, results showed that felodipine could effectively inhibit the growth of MRSE. Bioact Mater. 2021 Nov 24;14:272-289.
MRSA (ATCC 43300) 8 μg/mL 24 hours Evaluate the antibacterial effect of felodipine on MRSA, results showed that felodipine could effectively inhibit the growth of MRSA. Bioact Mater. 2021 Nov 24;14:272-289.
Brain tissue 1.0 nM 30 minutes Measure the effect of Felodipine on [3H]-isradipine binding in brain tissue. Results showed that Felodipine significantly inhibited [3H]-isradipine binding. Br J Pharmacol. 1994 Aug;112(4):1017-24.
LL29 cells 6 µM and above 48 hours Inhibited TGF-β1-induced collagen production without affecting cell viability Sci Rep. 2017 Jun 13;7(1):3439.
Mouse primary cortical neurons 1 µM and 5 µM 5 hours Felodipine increased LC3-II levels, indicating enhanced autophagic flux. Nat Commun. 2019 Apr 18;10(1):1817.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Spontaneously hypertensive rats (SHR) Spontaneously hypertensive rat model Subcutaneous osmotic minipump 0.4 mg/kg/day Once daily for four weeks Felodipine monotherapy decreased systolic blood pressure. The combination with ramipril was more effective than ramipril alone but not significantly better than felodipine monotherapy. The beneficial effect of felodipine monotherapy on left ventricular hypertrophy was less prominent than that of ramipril, but its cardioprotective effect was improved when combined with ramipril. Br J Pharmacol. 1997 Jun;121(3):503-10
Mice Ethanol dependence model Intraperitoneal injection 10 mg/kg Single dose Evaluate the effect of Felodipine on the ethanol withdrawal syndrome. Results showed that Felodipine did not significantly alter the behavioral manifestations of ethanol withdrawal. Br J Pharmacol. 1994 Aug;112(4):1017-24.
CD1 ICR mice Skin and soft tissue infection model Subcutaneous injection 20 mg/kg and 40 mg/kg Every 24 hours for 7 days Evaluate the antibacterial effect of felodipine in a murine skin and soft tissue infection model, results showed that high-dose felodipine significantly reduced fluorescence intensity and bacterial burden at the infection site. Bioact Mater. 2021 Nov 24;14:272-289.
ICR mice Bleomycin-induced pulmonary fibrosis model Intratracheal administration 3.3 mg/kg Once daily for 14 days Prevented and treated bleomycin-induced pulmonary fibrosis, improved lung function and reduced collagen deposition Sci Rep. 2017 Jun 13;7(1):3439.
Mice B6HD (N171-82Q) mice Intraperitoneal injections 5 mg/kg Three times a week for 6 weeks Felodipine improved motor performance and reduced huntingtin aggregate numbers in B6HD mice. Nat Commun. 2019 Apr 18;10(1):1817.
Mice P301S transgenic mice (PS19) Intraperitoneal injection 5 mg/kg Daily for 14 days Felodipine significantly attenuated tau-mediated microglial activation and NLRP3 expression, and significantly reduced tau hyperphosphorylation at S202/Thr205 and Thr212/Ser214 residues by inhibiting JNK/P38 signaling. Mol Brain. 2024 Sep 2;17(1):62
Wistar-Kyoto rats Fructose-fed rat model Intubation 5 mg/kg/day Once daily for 6 weeks Felodipine significantly attenuated the increased levels in serum IL-18 and cardiac IL-18 mRNA as well as coronary perivascular fibrosis in fructose-fed rats. Mol Med. 2008 Jul-Aug;14(7-8):395-402

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.02mL

5.20mL

2.60mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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