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Chemical Structure| 68099-86-5 Chemical Structure| 68099-86-5

Structure of Bepridil HCl
CAS No.: 68099-86-5

Chemical Structure| 68099-86-5

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Bepridil hydrochloride (CERM 1978) is a calcium channel inhibitor with anti-anginal effects.

Synonyms: CERM 1978; Bepridil (hydrochloride); Bepridil hydrochloride

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Product Details of Bepridil HCl

CAS No. :68099-86-5
Formula : C24H35ClN2O
M.W : 403.00
SMILES Code : CC(C)COCC(N1CCCC1)CN(C2=CC=CC=C2)CC3=CC=CC=C3.[H]Cl
Synonyms :
CERM 1978; Bepridil (hydrochloride); Bepridil hydrochloride
MDL No. :MFCD00065498
InChI Key :JXBBWYGMTNAYNM-UHFFFAOYSA-N
Pubchem ID :50088

Safety of Bepridil HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human cardiac thin filaments 100 μM Bepridil significantly increased the Ca2+-sensitivity of human cardiac thin filaments and uncoupled the relationship between Ca2+-sensitivity and TnI phosphorylation level. Cardiovasc Res. 2015 Oct 1;108(1):99-110
Primary neurons (Tg2576 mice) 5-30 μM 24 h Bepridil inhibited Aβ and APPsβ generation. J Neurosci. 2010 Jun 30;30(26):8974-83
H4 and U373 cells 5-30 μM 4 h Bepridil inhibited the generation of APPsβ. J Neurosci. 2010 Jun 30;30(26):8974-83
293T cells 10 μM 72 h Evaluate the cellular inhibition effect of Bepridil on SARS-CoV-2 main protease (MPro), results showed Bepridil has weak to undetectable cellular MPro inhibition potency. ACS Cent Sci. 2022 Feb 23;8(2):192-204
A549/ACE2 6.25 μM 4 days To evaluate the antiviral activity of Bepridil against SARS-CoV-2, results showed that Bepridil completely inhibited virus-induced cytopathic effect (CPE) at low micromolar concentrations. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10):e2012201118
fast skeletal muscle fibres 100 μM To investigate the effect of Bepridil on Ca2+ affinity of TnC in fast skeletal muscle fibres, results showed that Bepridil increased Ca2+ affinity of TnC, but the reactivity was lower than in slow fibres. Br J Pharmacol. 1999 Oct;128(3):767-73
slow skeletal muscle fibres 100 μM To investigate the effect of Bepridil on Ca2+ affinity of TnC in slow skeletal muscle fibres, results showed that Bepridil increased Ca2+ affinity of TnC, and slow fibres were more reactive to the drug than fast fibres. Br J Pharmacol. 1999 Oct;128(3):767-73
Vero E6 cells 0.16–20 µM 48 h To evaluate the inhibitory effect of Bepridil on Marburg virus, results showed that Bepridil inhibited MARV replication with an IC50 of 5.99±1.05 µM. J Infect Dis. 2018 Nov 22;218(suppl_5):S588-S591
HEK293-APPswe cells 5-30 μM 16 h Bepridil reduced total Aβ levels and modulated the cleavage specificity of γ-secretase. J Neurosci. 2010 Jun 30;30(26):8974-83
HEK293-APP cells 5-30 μM 4 h Bepridil inhibited the generation of APPsβ and Aβ with an IC50 of ~16 μM. J Neurosci. 2010 Jun 30;30(26):8974-83

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Marburg virus infection model Intraperitoneal injection 12 mg/kg Once or twice daily for 10 days To evaluate the therapeutic effect of Bepridil on Marburg virus-infected mice, results showed 80% and 90% survival rates with once and twice daily dosing, respectively. J Infect Dis. 2018 Nov 22;218(suppl_5):S588-S591

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.41mL

2.48mL

1.24mL

24.81mL

4.96mL

2.48mL

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
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

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