| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Through competitive binding assays, P1075 (3 nM) causes a monophasic inhibition curve in the presence of MgATP [1]. In rabbit cardiomyocytes, P1075 (100 µM; 10 min) produces ROS in a KATP-dependent way [2]. In isolated rabbit hearts, P1075 (150 nM) decreased the extent of infarcts when compared to control animals (area at risk: 10.6% vs. 31.5%, P < 0.05) [2].
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|---|---|
| ln Vivo |
In ischemia models, P1075 (iv; 1 μg/kg; once) therapy resulted in a smaller infarct [3].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: COS-7 Cell Tested Concentrations: 3-15 nM Incubation Duration: Experimental Results: The IC50 value is 15 nM and the Hill coefficient is 1.0. Cell viability assay [2] Cell Types: Adult rabbit cardiomyocytes Tested Concentrations: 100 µM Incubation Duration: 10 minutes Experimental Results: Resulted in a 44% increase in ROS production (P<0.001 compared to untreated cells). |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, ischemia for 30 minutes, reperfusion for 2 hrs (hrs (hours)) [3]
Doses: 1μg/kg Route of Administration: intravenous (iv) (iv)injection; reperfusion after 2 hrs (hrs (hours)). 1 microgram/kg; Experimental Results: Infarct size was diminished (41.8%) compared to vehicle. |
| References |
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| Additional Infomation |
1-cyano-2-(2-methylbutan-2-yl)-3-(3-pyridinyl)guanidine is a member of pyridines.
|
| Molecular Formula |
C12H17N5
|
|---|---|
| Molecular Weight |
231.3
|
| Exact Mass |
231.148
|
| CAS # |
60559-98-0
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| PubChem CID |
43345
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| Appearance |
White to off-white solid powder
|
| Density |
1.07g/cm3
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| Boiling Point |
347.6ºC at 760 mmHg
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| Melting Point |
186-187 °C
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| Flash Point |
164.1ºC
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| Index of Refraction |
1.556
|
| LogP |
2.572
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
17
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| Complexity |
312
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
HKZNADVVGXKQDL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H17N5/c1-4-12(2,3)17-11(15-9-13)16-10-6-5-7-14-8-10/h5-8H,4H2,1-3H3,(H2,15,16,17)
|
| Chemical Name |
1-cyano-2-(2-methylbutan-2-yl)-3-pyridin-3-ylguanidine
|
| Synonyms |
U-83757; PNU-83757; P-1075
|
| 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 : ~250 mg/mL (~1080.85 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.99 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 (8.99 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 (8.99 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 | 4.3234 mL | 21.6169 mL | 43.2339 mL | |
| 5 mM | 0.8647 mL | 4.3234 mL | 8.6468 mL | |
| 10 mM | 0.4323 mL | 2.1617 mL | 4.3234 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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