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PSI-697 (PSI697; PSI 697)is a novel, orally bioavailable, and non-carbohydrate-based P-selectin inhibitor (IC50 = 125 μM) derived from a series of tetrahydrobenzoquinoline salicylic. It may be used for atherothrombotic and venous thrombotic indications. P-selectin plays a key and well documented role in vascular disease by mediating leukocyte and platelet rolling and adhesion.
| ln Vitro |
It was determined that PSI-697 would block 50% of binding at 125 μM [1].
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| ln Vivo |
In comparison to vascular platforms, PSI-697 (0-50 mg/kg; channel) dramatically lowers rolling leukocyte counts by 39% [1]. In a vascular venous thrombosis model, PSI-697 (100 mg/kg; Channel) decreases thrombus weight by 18% in comparison to arterial material without lengthening the thrombosis period [1]. In a baboon model of vasculogenesis, PSI-697 (30 mg/kg; Manhattan daily; 6 days) reduces blood vessels and increases thrombolysis. In a model of wall damage, PSI-697 (30 mg/kg; ig; daily) decreases venous thrombosis and venous stenosis.
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| Animal Protocol |
Animal/Disease Models: 4-5 weeks male SD (SD (Sprague-Dawley)) rat (50-100 g)[1]
Doses: 0 mg/kg, 30 mg/kg, 50 mg/kg Route of Administration: Oral Experimental Results: The number of rolling leukocytes was diminished by 39% at the oral dose of 50 mg/kg compared to vehicle control. |
| References |
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| Additional Infomation |
PSI-697 has been used in trials studying the treatment of Scleritis.
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| Molecular Formula |
C21H18CLNO3
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| Molecular Weight |
367.829
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| Exact Mass |
367.098
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| CAS # |
851546-61-7
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| PubChem CID |
12004316
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.761
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DIEPFYNZGUUVHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18ClNO3/c22-14-8-5-12(6-9-14)11-17-20(24)18(21(25)26)16-10-7-13-3-1-2-4-15(13)19(16)23-17/h5-10,24H,1-4,11H2,(H,25,26)
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| Chemical Name |
2-[(4-chlorophenyl)methyl]-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid
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| Synonyms |
PSI 697 PSI697 PSI-697
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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 : ≥ 45.8 mg/mL (~124.51 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7186 mL | 13.5932 mL | 27.1865 mL | |
| 5 mM | 0.5437 mL | 2.7186 mL | 5.4373 mL | |
| 10 mM | 0.2719 mL | 1.3593 mL | 2.7186 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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