| 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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| Targets |
The primary target of NVP-VID-400 is CYP51, a cytochrome P450 enzyme that is essential for sterol biosynthesis in trypanosomes. It acts as a potent inhibitor of T. cruzi and T. brucei CYP51. It also inhibits CYP24A1. By inhibiting CYP51, it disrupts sterol synthesis in the parasites, leading to their death.
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| ln Vitro |
In vitro, NVP-VID-400 inhibits T. cruzi CYP51 with an I/E2(60 min) of 9 and T. brucei CYP51 with an I/E2(60 min) of 35. The I/E2a(5 min) values for both parasites are <1. These values indicate the compound's potent inhibitory activity against the parasite enzymes. It is a selective inhibitor of protozoal CYP51 over mammalian CYP51.
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| ln Vivo |
Treatment for human trypanosomiasis may be possible by the selective suppression of protozoal CYP51 [1].
In vivo, NVP-VID-400 has been studied for the treatment of human trypanosomiasis by selective suppression of protozoal CYP51. This suggests that the compound is effective in animal models of Chagas disease and African sleeping sickness. Its oral bioavailability and efficacy in vivo make it a promising lead compound for the development of new anti-trypanosomal therapies. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for NVP-VID-400 involve CYP51 inhibition assays using recombinant T. cruzi or T. brucei CYP51 enzymes. The compound's inhibitory activity is measured by monitoring the metabolism of a substrate (e.g., 14α-methyl sterols) in the presence of NADPH. I/E2 values (the ratio of inhibitor concentration to enzyme concentration required for 50% inhibition at a given time) are used to quantify potency.
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| Cell Assay |
In vitro cellular assays for NVP-VID-400 are conducted in cultures of T. cruzi or T. brucei parasites. The compound's anti-parasitic activity is assessed by measuring parasite growth inhibition or viability. IC50 values are determined from dose-response curves. Its selectivity for parasite vs. mammalian cells can be evaluated using mammalian cell lines to assess cytotoxicity.
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| Animal Protocol |
In vivo animal studies for NVP-VID-400 are conducted in mouse models of T. cruzi or T. brucei infection. Animals are administered the compound orally or intraperitoneally, and parasite burden in blood and tissues is monitored over time. The compound's efficacy is assessed by measuring survival rates and reduction in parasitemia. Its ability to cure established infections is evaluated in these models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NVP-VID-400 indicate it has a molecular weight of 401.89 and a molecular formula of C24H20ClN3O. It is soluble in DMSO at 15 mg/mL. For in vivo administration, it can be formulated as a homogeneous suspension in CMC-Na for oral dosing. The compound is stable as a powder and should be stored at appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicological information for NVP-VID-400 is derived from preclinical studies. As a CYP51 inhibitor, it may have effects on sterol metabolism in the host, although its selectivity for protozoal CYP51 is intended to minimize these effects. Comprehensive toxicology studies would be required for clinical development, including assessments of hepatic, endocrine, and reproductive toxicity.
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| References | |
| Additional Infomation |
NVP-VID-400 is a research compound with potential for the treatment of human trypanosomiasis. It is also known as SDZ285428. It is a potent inhibitor of CYP51 from T. cruzi and T. brucei. The compound is available from research chemical suppliers for preclinical studies. It is not approved for clinical use.
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| Molecular Formula |
C24H20CLN3O
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|---|---|
| Molecular Weight |
401.894
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| Exact Mass |
401.129
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| CAS # |
174262-13-6
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| Related CAS # |
174262-13-6;
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| PubChem CID |
9952928
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
651.2±55.0 °C at 760 mmHg
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| Flash Point |
347.7±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
4.54
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C(CNC(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)Cl)N4C=CN=C4
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| InChi Key |
FHHNSSGZEIVGMS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H20ClN3O/c25-22-12-10-19(11-13-22)18-6-8-21(9-7-18)24(29)27-16-23(28-15-14-26-17-28)20-4-2-1-3-5-20/h1-15,17,23H,16H2,(H,27,29)
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| Chemical Name |
N-(2-(1H-imidazol-1-yl)-2-phenylethyl)-4'-chloro-[1,1'-biphenyl]-4-carboxamide
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| Synonyms |
NVP-VID-400 NVP-VID 400 NVP-VID400 SDZ285428 SDZ 285428 SDZ-285428 SDZ285-428 SDZ 285-428 SDZ-285-428.
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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 |
| 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 : ~50 mg/mL (~124.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4882 mL | 12.4412 mL | 24.8824 mL | |
| 5 mM | 0.4976 mL | 2.4882 mL | 4.9765 mL | |
| 10 mM | 0.2488 mL | 1.2441 mL | 2.4882 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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