| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
Many advantageous pleiotropic effects of OR-1896 have been demonstrated by a growing body of evidence. Considerable vasodilation is induced by OR-1896, and a potent vasodilatory mechanism appears to involve the activation of ATP-sensitive sarcolemmal K+ channels in smooth muscle cells. Activating ATP-sensitive K+ channels in mitochondria can also suggest pharmacological strategies for cardioprotection and broaden the range of controls available to the cell to govern mitochondrial ATP generation [1].
|
|---|---|
| ln Vivo |
Levosimendan is metabolized by the large intestine, where about 5% of the drug is transformed into the metabolite OR-1855. The metabolite OR-1896 is then formed by acetylation in the liver. OR-1896 is only 40% bound to plasma proteins, compared to 98% binding for levosimendan. The elimination half-life of OR-1896 is roughly 75 to 80 hours, allowing cardiovascular effects to last for up to 7 to 9 days after ending the 24-hour infusion. This is in contrast to levosimendan, which has a half-life of 1-1.5 hours. The Zuo Ximendan. While the metabolite's (OR-1896) elimination can be extended, the parent drug's pharmacokinetics remain unchanged in persons with severe renal impairment or mild hepatic impairment [1].
|
| References | |
| Additional Infomation |
OR-1896 is an anilide and a member of acetamides.
|
| Molecular Formula |
C₁₃H₁₅N₃O₂
|
|---|---|
| Molecular Weight |
245.28
|
| Exact Mass |
245.116
|
| CAS # |
220246-81-1
|
| PubChem CID |
9816296
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.278 g/cm3
|
| Melting Point |
224-226ºC
|
| LogP |
1.342
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
370
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[C@@H]1CC(=O)NN=C1C2=CC=C(C=C2)NC(=O)C
|
| InChi Key |
GDZXNMWZXLDEKG-MRVPVSSYSA-N
|
| InChi Code |
InChI=1S/C13H15N3O2/c1-8-7-12(18)15-16-13(8)10-3-5-11(6-4-10)14-9(2)17/h3-6,8H,7H2,1-2H3,(H,14,17)(H,15,18)/t8-/m1/s1
|
| Chemical Name |
N-[4-[(4R)-4-methyl-6-oxo-4,5-dihydro-1H-pyridazin-3-yl]phenyl]acetamide
|
| Synonyms |
OR1896; OR 1896
|
| 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) |
DMSO : ~62.5 mg/mL (~254.81 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.48 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 (8.48 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 (8.48 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 | 4.0770 mL | 20.3849 mL | 40.7697 mL | |
| 5 mM | 0.8154 mL | 4.0770 mL | 8.1539 mL | |
| 10 mM | 0.4077 mL | 2.0385 mL | 4.0770 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
