| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vivo |
By interacting with TPO receptors on megakaryocytes, thrombopoietin (TPO) receptor agonists are novel therapies for patients with chronic ITP. These therapies can increase platelet counts, decrease bleeding events, and lessen the need for auxiliary or rescue treatment. Although TPO receptor agonists are well tolerated, there is still some confusion surrounding the possibility of myelofibrosis and thrombosis [2].
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| References |
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| Additional Infomation |
SB-559448 is a small-molecule drug that mimics the activity of thrombopoietin (TPO), a protein factor that promotes growth and production of blood platelets. This drug is developed by GlaxoSmithKline and used to treat Thrombocytopenia.Thrombocytopenia (decreased platelet count) is a common side effect of many chemotherapies and can lead to uncontrolled bleeding, thus representing a significant problem in the treatment of cancer patients.
Drug Indication Investigated for use/treatment in thrombocytopenia. |
| Molecular Formula |
C25H22N8O2
|
|---|---|
| Molecular Weight |
466.5
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| Exact Mass |
466.186
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| CAS # |
1033040-23-1
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| PubChem CID |
135451068
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| Appearance |
Pink to red solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
703.5±70.0 °C at 760 mmHg
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| Flash Point |
379.3±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.735
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| LogP |
3.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
834
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YLSNQYHZCMCURB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H22N8O2/c1-14-10-11-19(12-15(14)2)33-25(35)22(16(3)30-33)27-26-21-9-5-8-20(23(21)34)17-6-4-7-18(13-17)24-28-31-32-29-24/h4-13,30,34H,1-3H3,(H,28,29,31,32)
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| Chemical Name |
2-(3,4-dimethylphenyl)-4-[[2-hydroxy-3-[3-(2H-tetrazol-5-yl)phenyl]phenyl]diazenyl]-5-methyl-1H-pyrazol-3-one
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| Synonyms |
TPOAgonist1; TPO Agonist 1; TPO-Agonist-1
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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 : ≥ 36 mg/mL (~77.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.29 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 20.0 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 mg/mL (4.29 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1436 mL | 10.7181 mL | 21.4362 mL | |
| 5 mM | 0.4287 mL | 2.1436 mL | 4.2872 mL | |
| 10 mM | 0.2144 mL | 1.0718 mL | 2.1436 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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