| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
BMS-919373 primarily targets the Kv1.5 potassium channel (KCNA5), which mediates the ultra-rapid delayed rectifier potassium current (IKur). IKur is a key repolarizing current in the human atrium. By blocking IKur, BMS-919373 prolongs the atrial action potential duration and refractory period, which can terminate or prevent atrial fibrillation. It has an IC50 of 50 nM for IKur blockade.
|
|---|---|
| ln Vitro |
In vitro, BMS-919373 is a selective and potent IKur current blocker with an IC50 of 50 nM. Its activity is characterized by its ability to block Kv1.5 channels and inhibit IKur currents in electrophysiological assays. Its selectivity for IKur over other cardiac potassium channels is a key feature of its profile. The compound can be used for the research of cardiovascular diseases.
|
| ln Vivo |
In vivo, BMS-919373 is being developed for the treatment of atrial fibrillation and acute coronary syndrome. Phase II development is underway in the US and Canada for paroxysmal atrial fibrillation. By blocking IKur, it may effectively treat atrial fibrillation without affecting ventricular repolarization, potentially offering a safer alternative to existing antiarrhythmic drugs.
|
| Enzyme Assay |
The in vitro activity of BMS-919373 is assessed using electrophysiological techniques, such as the patch-clamp technique. Cells expressing Kv1.5 channels are voltage-clamped, and IKur currents are elicited by depolarizing voltage steps. Various concentrations of BMS-919373 are applied, and the inhibition of the IKur current is measured to determine the IC50. For selectivity profiling, the compound is tested against other potassium channels.
|
| Cell Assay |
For cellular assays, cells expressing Kv1.5 channels (e.g., CHO or HEK293 cells transfected with KCNA5) are cultured in appropriate media. Cells are treated with various concentrations of BMS-919373 (typically 1-1000 nM) for defined periods. IKur currents are measured using patch-clamp electrophysiology. Cell viability is assessed using standard assays.
|
| Animal Protocol |
In vivo, BMS-919373 is typically administered orally to animal models of atrial fibrillation. In preclinical studies, the compound is administered at various doses, and its effects on atrial refractoriness and the induction of atrial fibrillation are assessed. In clinical trials, the compound is administered to patients with paroxysmal atrial fibrillation, and efficacy is assessed by measuring the reduction in atrial fibrillation episodes.
|
| ADME/Pharmacokinetics |
BMS-919373 has a molecular weight of 468.53 g/mol and a molecular formula of C25H20N6O2S. It is a selective, potent IKur current blocker. The compound should be stored as a powder at -20°C under desiccated conditions. Specific solubility and pharmacokinetic parameters are not detailed in the provided search results. It is soluble in DMSO and other organic solvents.
|
| Toxicity/Toxicokinetics |
BMS-919373 can cause side effects related to its mechanism of action, including potential effects on cardiac electrophysiology. The compound is intended for clinical use under appropriate regulatory oversight. Comprehensive toxicological studies are required to establish its full safety profile. Standard laboratory safety precautions should be followed when handling the compound.
|
| Additional Infomation |
BMS-919373 is being studied in the clinical trial NCT02153437 (using a pacemaker to study the effects of BMS-919373 on cardiac electrical activity).
BMS-919373 is a selective, potent IKur current blocker and a potassium channel Kv1.5 (KCNA5) inhibitor. It has an IC50 of 50 nM for IKur blockade. BMS-919373 is being developed for the treatment of atrial fibrillation and acute coronary syndrome. Phase II development is underway for paroxysmal atrial fibrillation. The compound is not approved for clinical use and is intended for research purposes. |
| Molecular Formula |
C25H20N6O2S
|
|---|---|
| Molecular Weight |
468.535
|
| Exact Mass |
468.136
|
| CAS # |
1272353-82-8
|
| Related CAS # |
1272353-82-8;
|
| PubChem CID |
51030730
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
662.6±65.0 °C at 760 mmHg
|
| Flash Point |
354.5±34.3 °C
|
| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.703
|
| LogP |
2.62
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
34
|
| Complexity |
755
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1=CN=CC(=C1)C1=NC2=CC=CC(C3C=CC=CC=3)=C2C(=N1)NCC1C=CC=CN=1)(N)(=O)=O
|
| InChi Key |
XGKULQQVQWCASY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H20N6O2S/c26-34(32,33)20-13-18(14-27-16-20)24-30-22-11-6-10-21(17-7-2-1-3-8-17)23(22)25(31-24)29-15-19-9-4-5-12-28-19/h1-14,16H,15H2,(H2,26,32,33)(H,29,30,31) SMILES
|
| Chemical Name |
5-(5-phenyl-4-((pyridin-2-ylmethyl)amino)quinazolin-2-yl)pyridine-3-sulfonamide
|
| Synonyms |
BMS-919373 BMS 919373 BMS919373.
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1343 mL | 10.6714 mL | 21.3429 mL | |
| 5 mM | 0.4269 mL | 2.1343 mL | 4.2686 mL | |
| 10 mM | 0.2134 mL | 1.0671 mL | 2.1343 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA