Art. -Nr.: HY-50722

NNC 55-0396

(Synonyms: NNC 55-0396 dihydrochloride)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

NNC 55-0396 (NNC 55-0396 dihydrochloride) is a blood-brain-barrier-permeable T-type Ca²⁺ channel inhibitor and pan-P450 inhibitor. NNC 55-0396 selectively inhibits T-type Ca²⁺ channels, suppresses HIF-1α expression and stability and inhibits Kv currents. NNC 55-0396 reduces brain infarct and attenuates neurological dysfunction. NNC 55-0396 inhibits the activity of multiple P450 enzymes. NNC 55-0396 (free base) can be used for the research of brain injury, hypertension, and glioblastoma.

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Reinheit: 98.43%
CAS. Nr.: 357400-13-6
Formel: C₃₀H₄₀Cl₂FN₃O₂
Molecular Weight:564.56

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

NNC 55-0396 Chemical Structure

CAS. Nr.: 357400-13-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]^[3]

CYP3A4

300 nM (IC₅₀)

CYP3A4

210 nM (Ki)

CYP2D6

29 nM (IC₅₀)

CYP2D6

2.8 nM (Ki)

T-type calcium channel

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

In Vitro

NNC 55-0396 potently inhibits recombinant human CYP3A4 and CYP2D6 at 100 nM and 10 μM, with weaker or no inhibition of recombinant human CYP1A2, CYP2E1, CYP2C9, CYP2C19, and CYP2C8 at these concentrations^[2].
NNC 55-0396 inhibits recombinant human CYP3A4 BFC debenzylation activity with an IC₅₀ of 300 nM and a K_i of 210 nM^[2].
NNC 55-0396 inhibits recombinant human CYP2D6 AMMC N-demethylation activity with an IC₅₀ of 29 nM and a K_i of 2.8 nM^[2].
NNC 55-0396 inhibits CYP3A4-mediated testosterone 6β-hydroxylase activity in human liver microsomes with an IC₅₀ of 11.0 μM and a K_i of 3.9 μM^[2].
NNC 55-0396 inhibits CYP2D6-mediated harmaline metabolism in human liver microsomes with an IC₅₀ of 72.6 nM and a K_i of 57.1 nM^[2].
NNC 55-0396 (1-20 μM; 72 h) inhibits the growth of HepG2 cells more potently in galactose medium than glucose medium^[3].
NNC 55-0396 (1-5 μM; 5 h) dose-dependently inhibits hypoxia-induced HIF-1α protein stability in HepG2 cells, with a near-complete reduction at 5 μM after 4 h hypoxic incubation, without affecting HIF-1β levels^[3].
NNC 55-0396 (1-5 μM; 5 h) dose-dependently increases the hydroxylation of HIF-1α in HepG2 cells under hypoxic conditions, with a 6-fold increase observed at 5 μM after 4 h incubation^[3].
NNC 55-0396 (1-5 μM; 5 h) reduces hypoxia-induced mitochondrial ROS levels in HepG2 cells^[3].
NNC 55-0396 (1 μM) decreases the half-life of hypoxia-stabilized HIF-1α in HepG2 cells, reducing it from over 80 minutes to less than 70 minutes^[3].
NNC 55-0396 (1-5 μM; 5 h) inhibits Desferrioxamine-induced HIF-1α stabilization in HepG2 cells, with a 50% reduction observed at 5 μM after 4 h incubation^[3].
NNC 55-0396 (1-5 μM; 75 min) reduces hypoxia-induced HIF-1α protein levels in HepG2 cells, with significant suppression observed at 1 μM and 5 μM^[3].
NNC 55-0396 (1-5 μM; 75 min) inhibits hypoxia-induced phosphorylation of mTOR and p70S6K in HepG2 cells, with a 70% reduction in phospho-mTOR levels observed at 5 μM after 15 min hypoxic incubation^[3].
NNC 55-0396 (1-5 μM; 17 h) dose-dependently reduces hypoxia-induced VEGF expression in HepG2 cells, with significant suppression observed at 1 μM and 5 μM after 16 h hypoxic incubation^[3].
NNC 55-0396 (0.001-10 mM; 1 min) dose-dependently inhibits K_v currents in freshly isolated rabbit coronary arterial smooth muscle cells with an IC₅₀ of 0.08 mM^[4].
NNC 55-0396 potently blocks recombinant Cav3.1 T-type calcium channels in HEK293 cells with an IC₅₀ of 6.8 μM, via a state-dependent^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

human liver carcinoma HepG2 cells
Concentration:

1 μM; 2 μM; 5 μM; 7 μM; 10 μM; 20 μM
Incubation Time:

72 h
Result:

Exhibited stronger inhibitory effects on cell growth in galactose medium than in glucose medium.
Increased glucose/galactose cell growth ratios significantly at concentrations of 5, 7, 10, and 20 μM.

Western Blot Analysis^[3]

Cell Line:

human liver carcinoma HepG2 cells
Concentration:

1 μM; 5 μM
Incubation Time:

5 h
Result:

Suppressed hypoxia-induced HIF-1α protein stability in a dose-dependent manner, with no effect on HIF-1β stability.
Reduced HIF-1α expression to ~80% of hypoxic control levels at 1 μM.
Reduced HIF-1α expression to ~20% of hypoxic control levels at 5 μM (p<0.001).\nIncreased the ratio of hydroxy-HIF-1α to total HIF-1α in a dose-dependent manner.
Increased the ratio to ~250% of control levels at 1 μM.
Increased the ratio to ~600% of control levels at 5 μM (p<0.001).

Western Blot Analysis^[3]

Cell Line:

human liver carcinoma HepG2 cells
Concentration:

1 μM; 5 μM
Incubation Time:

5 h
Result:

Inhibited DFO-induced HIF-1α stabilization.
Reduced HIF-1α expression to ~100% of DFO-treated control levels at 1 μM.
Reduced HIF-1α expression to ~50% of DFO-treated control levels at 5 μM (p<0.01).

Western Blot Analysis^[3]

Cell Line:

human liver carcinoma HepG2 cells
Concentration:

1 μM; 5 μM
Incubation Time:

75 min
Result:

Repressed hypoxia-induced phosphorylation of mTOR and p70S6K.
Reduced phospho-mTOR levels to 0.8-fold of hypoxic control levels at 1 μM.
Reduced phospho-mTOR levels to 0.3-fold of hypoxic control levels at 5 μM.
Reduced phospho-p70S6K levels to 0.9-fold and 0.8-fold of hypoxic control levels at 1 μM and 5 μM, respectively.

ELISA Assay^[3]

Cell Line:

human liver carcinoma HepG2 cells
Concentration:

1 μM; 5 μM
Incubation Time:

17 h
Result:

Decreased hypoxia-induced VEGF expression in a dose-dependent manner.
Reduced relative VEGF expression to ~220% of normoxic control levels at 1 μM (vs ~280% for hypoxic control; p<0.01).
Reduced relative VEGF expression to ~180% of normoxic control levels at 5 μM (p<0.01).

In Vivo

NNC 55-0396 (5-20 mg/kg; i.p.; 2 doses) significantly reduces MCAO/R-induced ischemic brain injury and associated neurological dysfunctions^[1].
NNC 55-0396 (10-20 mg/kg; i.p.; every 2 days for 20 days) significantly reduces glioblastoma tumor weight by 40-60% and suppresses tumor angiogenesis via reduced HIF-1α, VEGF, and PECAM-1 expression in a subcutaneous mouse xenograft model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

ddY mice (male, 3 weeks old, acclimated for a few weeks before experiments)^[1]
Dosage:

5 mg/kg; 20 mg/kg
Administration:

i.p.; 2 doses
Result:

Reduced MCAO/R-induced infarct area (at all measured distances from bregma) and infarct volume to ~30 mm³ (5 mg/kg i.p. pre-occlusion) and ~45 mm³ vs. vehicle ~70 mm³.
Tended to attenuate some neurological dysfunctions, including increased test latency in the passive avoidance test and reduced time spent in right-biased bending.

Animal Model:

BALB/c-nu/nu (athymic nude) (4-week-old female, subcutaneous glioblastoma xenograft model)^[3]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; every 2 days for 20 days
Result:

Reduced xenograft tumor volume and weight relative to vehicle controls.
Significantly reduced tumor weight (p<0.01 for 10 mg/kg, p<0.001 for 20 mg/kg).
Significantly reduced HIF-1α, VEGF, and PECAM-1 expression levels in tumor tissue.
Significantly decreased microvessel density (p<0.001 for 10 mg/kg, p<0.01 for 20 mg/kg).
Caused no weight loss or liver toxicity in treated mice.

Chemical Information

CAS. Nr. 357400-13-6
Appearance Solid
Molecular Weight 564.56
Formel C₃₀H₄₀Cl₂FN₃O₂
Color Off-white to yellow
SMILES

O=C(C1CC1)O[C@@]2(CCN(CCCC3=NC4=CC=CC=C4N3)C)[C@@H](C(C)C)C5=C(C=C(F)C=C5)CC2.[H]Cl.[H]Cl
Synonyms

NNC 55-0396 dihydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (6)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

Cell Death Differ

MARCH8/NSUN6/ROS-mediated DNA damage positive feedback loop regulates cisplatin resistance in osteosarcoma. [Abstract]

2025 Jul 19. PMID: 40683951
Br J Pharmacol

Endothelium-derived hydrogen sulfide acts as a hyperpolarizing factor and exerts neuroprotective effects via activation of large-conductance Ca2+ -activated K+ channels. [Abstract]

2021 Oct;178(20):4155-4175. PMID: 34216027

NNC 55-0396 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Oct;178(20):4155-4175. [Abstract]

Effect of NaHS on neuronal viability against OGD/R injury in vitro. Cell viability was measured by CCK-8 at 24 h post-reoxygenation. Data: mean ± SD, n=6. #P<0.05 vs Normal; *P<0.05 vs Model (OGD/R); &P<0.05 vs NaHS (1 µM); $P<0.05 vs BMS-191011 (BMS) (10 µM); %P<0.05 vs NaHS+Verapamil (Ver) (100 µM); ※P<0.05 vs Verapamil alone. NNC 55-0396 (NNC): 100 µM.

NNC 55-0396 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Oct;178(20):4155-4175. [Abstract]

Effect of NaHS on neuronal viability against OGD/R injury in vitro. Cell viability was measured by CCK-8 at 24 h post-reoxygenation. Data: mean ± SD, n=6. #P<0.05 vs Normal; *P<0.05 vs Model (OGD/R); &P<0.05 vs NaHS (1 µM); $P<0.05 vs BMS-191011 (BMS) (10 µM); %P<0.05 vs NaHS+Verapamil (Ver) (100 µM); ※P<0.05 vs Verapamil alone. NNC 55-0396 (NNC): 100 µM.
Int J Mol Sci

Alkaline Dilution Alters Sperm Motility in Dairy Goat by Affecting sAC/cAMP/PKA Pathway Activity. [Abstract]

2023 Jan 16;24(2):1771. PMID: 36675287
Fish Physiol Biochem

The voltage-gated T-type Ca2+ channel is key to the sperm motility of Atlantic salmon (Salmo salar). [Abstract]

2020 Oct;46(5):1825-1831. PMID: 32506186
J Reprod Dev

Estradiol enhances T-type calcium channel activation in human myometrium telocytes. [Abstract]

2023 Apr 3;69(2):87-94. PMID: 36754390
bioRxiv

2026 Jun 24.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (177.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 50 mg/mL (88.56 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7713 mL

8.8565 mL

17.7129 mL

5 mM

0.3543 mL

1.7713 mL

3.5426 mL

10 mM

0.1771 mL

0.8856 mL

1.7713 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Matsuda S, et al. NNC 55-0396, a T-type calcium channel blocker, protects against the brain injury induced by middle cerebral artery occlusion and reperfusion in mice. J Pharmacol Sci. 2019;140(2):193-196. [Content Brief]

[2]. Bui PH, et al. The mibefradil derivative NNC55-0396, a specific T-type calcium channel antagonist, exhibits less CYP3A4 inhibition than mibefradil. Drug Metab Dispos. 2008;36(7):1291-1299. [Content Brief]

[3]. Kim KH, et al. NNC 55-0396, a T-type Ca2+ channel inhibitor, inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction. J Mol Med (Berl). 2015;93(5):499-509. [Content Brief]

[4]. Son YK, et al. Ca2+ channel inhibitor NNC 55-0396 inhibits voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells. J Pharmacol Sci. 2014;125(3):312-319. [Content Brief]

[5]. Li M, et al. Towards selective antagonists of T-type calcium channels: design, characterization and potential applications of NNC 55-0396. Cardiovasc Drug Rev. 2005;23(2):173-196. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.7713 mL	8.8565 mL	17.7129 mL	44.2823 mL
	5 mM	0.3543 mL	1.7713 mL	3.5426 mL	8.8565 mL
	10 mM	0.1771 mL	0.8856 mL	1.7713 mL	4.4282 mL
	15 mM	0.1181 mL	0.5904 mL	1.1809 mL	2.9522 mL
	20 mM	0.0886 mL	0.4428 mL	0.8856 mL	2.2141 mL
	25 mM	0.0709 mL	0.3543 mL	0.7085 mL	1.7713 mL
	30 mM	0.0590 mL	0.2952 mL	0.5904 mL	1.4761 mL
	40 mM	0.0443 mL	0.2214 mL	0.4428 mL	1.1071 mL
	50 mM	0.0354 mL	0.1771 mL	0.3543 mL	0.8856 mL
	60 mM	0.0295 mL	0.1476 mL	0.2952 mL	0.7380 mL
	80 mM	0.0221 mL	0.1107 mL	0.2214 mL	0.5535 mL
DMSO	100 mM	0.0177 mL	0.0886 mL	0.1771 mL	0.4428 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.

Keywords

NNC 55-0396

6 Cited Publications

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NNC 55-0396

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Mitochondria-Targeted Compound Library

Calcium Channel Blocker Library

Anti-Prostate Cancer Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NNC 55-0396

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NNC 55-0396

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Mitochondria-Targeted Compound Library

Calcium Channel Blocker Library

Anti-Prostate Cancer Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NNC 55-0396

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NNC 55-0396 Related Classifications

HY-50722 Related Classifications