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| 25mg |
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| 100mg |
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NQ301 is a synthetic 1,4-naphthoquinone derivative that acts as a selective CD45 inhibitor, displaying potent antithrombotic/antiplatelet activity. It exerts its antiplatelet activity by inhibiting collagen-challenged rabbit platelet aggregation with IC50 of 10 mg/mL.
| ln Vitro |
Rabbit platelet aggregation in response to collagen (10 mg/mL), U46619 (1 mg/mL), and arachidonic acid (100 mg/mL) challenges is inhibited by NQ301, with concentration-dependent IC50 values of 0.60±0.02, 0.58±0.04, and 0.78 ±0.04 μM, respectively. NQ301 has a concentration-dependent, potent suppression of thromboxane B2 formation by platelets exposed to arachidonic acid, but no effect on prostaglandin D2 production, suggesting that thromboxane A2 synthase is inhibited. In addition to modulating arachidonic acid liberation potential and the formation of 12-hydroxy-5,8,10,14-eicosatetraenoic acid in platelets, NQ301 has the ability to inhibit thromboxane A2 synthase activity through thromboxane A2/prostaglandin H2 receptor blockade[1]. Rather than directly preventing fibrinogen-GPIIb/IIIa complex binding, NQ301 suppresses the intracellular pathway to prevent platelet aggregation. In addition to markedly raising platelet cAMP levels in activated platelets, NQ301 also significantly reduces the rise in ATP secretion and cytosolic Ca2+ concentration. NQ301's antiplatelet action may be mediated by enhancing the production of cAMP, inhibiting ATP secretion in activated platelets, and blocking cytosolic Ca2+ mobilization[2].
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| References |
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| Molecular Formula |
C18H12CLNO3
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| Molecular Weight |
325.75
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| Exact Mass |
325.051
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| CAS # |
130089-98-4
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| Related CAS # |
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| PubChem CID |
781109
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LSQZKIQSQHZVQS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12ClNO3/c1-10(21)11-6-8-12(9-7-11)20-16-15(19)17(22)13-4-2-3-5-14(13)18(16)23/h2-9,20H,1H3
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.71 mg/mL (2.18 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0698 mL | 15.3492 mL | 30.6984 mL | |
| 5 mM | 0.6140 mL | 3.0698 mL | 6.1397 mL | |
| 10 mM | 0.3070 mL | 1.5349 mL | 3.0698 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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