| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
NNC 55-0396 dihydrochloride salt, an analog of mibefradil, is a novel, potent and highly selective T-type calcium channel blocker which displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. As a T-type calcium channel blocker, NNC 55-0396 inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction. NNC 55-0396 suppressed mitochondrial reactive oxygen species-mediated HIF-1α expression as well as stabilization by inhibiting protein synthesis in a dose-dependent manner. NNC 55-0396 inhibited tumor-induced angiogenesis in vitro and in vivo by suppressing HIF-1α stability. NNC 55-0396 could be a potential therapeutic drug candidate for cancer treatment.
| ln Vitro |
NNC 55-0396 (0.1-1000 μM) had no inhibitory effect on HVA Ca2+ current in INS-1 cells [1]. NNC 55-0396 (1-100 μM) The IC50 value of NNC 55-0396 boiling T-type Ca2+ current is 6.8 μM in HEK 293/α1G cells at a dose of 8 μM[1]. Boiled more than 50% of the T-type Ca2+ current [1].
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| ln Vivo |
In the cameline model and GABAA subunit α1 transcriptional dye, NNC 55-0396 (20 mg/kg; i.p. once) suppresses tremor [1].
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| Animal Protocol |
Animal/Disease Models: GABAA receptor α1 subunit-null mouse model [2]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; 20 mg/kg once Experimental Results: Inhibited tremor in GABAA subunit α1-deficient mice. |
| References |
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| Additional Infomation |
NNC 55-0396 dihydrochloride is the dihydrochloride salt of NNC 55-0396. It is a stable analogue of mibefradil and a highly selective T-type calcium channel blocker. It has a role as an antineoplastic agent, a neuroprotective agent, an apoptosis inducer, an angiogenesis inhibitor, a potassium channel blocker and a T-type calcium channel blocker. It contains a NNC 55-0396 (free base).
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| Molecular Formula |
C30H38FN3O2.2CLH
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|---|---|
| Molecular Weight |
564.56200
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| Exact Mass |
563.248
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| Elemental Analysis |
C, 63.82; H, 7.14; Cl, 12.56; F, 3.37; N, 7.44; O, 5.67
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| CAS # |
357400-13-6
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| Related CAS # |
(Rac)-NNC 55-0396;2517420-92-5
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| PubChem CID |
22084904
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| Appearance |
Off-white to yellow solid powder
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| Boiling Point |
713.8ºC at 760mmHg
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| Flash Point |
385.5ºC
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| LogP |
7.638
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
38
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| Complexity |
746
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| Defined Atom Stereocenter Count |
2
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| 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
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| InChi Key |
BCCQNBXHUMKLFW-HNQRYHMESA-N
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| InChi Code |
InChI=1S/C30H38FN3O2.2ClH/c1-20(2)28-24-13-12-23(31)19-22(24)14-15-30(28,36-29(35)21-10-11-21)16-18-34(3)17-6-9-27-32-25-7-4-5-8-26(25)33-27;;/h4-5,7-8,12-13,19-21,28H,6,9-11,14-18H2,1-3H3,(H,32,33);2*1H/t28-,30-;;/m0../s1
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| Chemical Name |
[(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] cyclopropanecarboxylate;dihydrochloride
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| Synonyms |
NNC 55-0396; NNC55-0396; NNC-55-0396; NNC-550396; NNC550396; NNC 550396; NNC 55-0396 dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~177.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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