| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
The Cmax, AUC0-∞, and t1/2 values for SRX246 (2 mg/kg; iv) therapy were 953 ng/mL and 1141 ng, respectively.For post-pharmacokinetics, the values are h/mL and 6.02 hours, respectively. (dosage 20 mg/kg), 98.4 ng/mL, 624 ng, and AUC0-∞ are the Cmax, AUC0-∞, and t1/2 values.m/mL and 2.38 hours, in that order [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [1].
Doses: 2 mg/kg (oral 20 mg/kg) Route of Administration: iv (pharmacokinetic/PK/PK analysis) Experimental Results: After iv administration, the plasma concentration diminished steadily, with a half-life (t1/2) of 6 hrs (hrs (hours)). The Cmax and AUC0-∞ values were 953 ng/mL, 1141 ng·h/mL, 6.02 hrs (hrs (hours)). After oral administration, the Cmax, AUC0-∞ and t1/2 values were 98.4 ng/mL, 624 ng·h/mL and 2.38 hrs (hrs (hours)) respectively. |
| References |
| Molecular Formula |
C42H49N5O5
|
|---|---|
| Molecular Weight |
703.868970632553
|
| Exact Mass |
703.373
|
| CAS # |
512784-93-9
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| PubChem CID |
44428550
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| Appearance |
White to off-white solid powder
|
| LogP |
5.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
52
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| Complexity |
1260
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1C(N([C@@H](C2C=CC=CC=2)C1)[C@@H]1C(N([C@@H](C(N[C@H](C)C2C=CC=CC=2)=O)CC(N2CCC(CC2)N2CCCCC2)=O)[C@@H]1/C=C/C1C=CC=CC=1)=O)=O
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| InChi Key |
FJUKOXWSIGULLE-JVOQCOEYSA-N
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| InChi Code |
InChI=1S/C42H49N5O5/c1-30(32-16-8-3-9-17-32)43-40(49)36(28-38(48)45-26-22-34(23-27-45)44-24-12-5-13-25-44)46-35(21-20-31-14-6-2-7-15-31)39(41(46)50)47-37(29-52-42(47)51)33-18-10-4-11-19-33/h2-4,6-11,14-21,30,34-37,39H,5,12-13,22-29H2,1H3,(H,43,49)/b21-20+/t30-,35-,36-,37-,39+/m1/s1
|
| Chemical Name |
(2R)-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-N-[(1R)-1-phenylethyl]-4-(4-piperidin-1-ylpiperidin-1-yl)butanamide
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| Synonyms |
SRX 246; SRX246; SRX-246
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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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~142.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.55 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 25.0 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: ≥ 2.5 mg/mL (3.55 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 25.0 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 | 1.4207 mL | 7.1036 mL | 14.2072 mL | |
| 5 mM | 0.2841 mL | 1.4207 mL | 2.8414 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4207 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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