| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
PAI-749 targets plasminogen activator inhibitor-1 (PAI-1), the primary physiological inhibitor of both tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA). PAI-749 binds directly to PAI-1, blocking PAI-1 from accessing the active site of tPA and abrogating formation of the SDS-stable tPA/PAI-1 complex. This preserves tPA and uPA activities, promoting fibrinolysis.
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| ln Vitro |
PAI-749 is a synthetic antagonist of plasminogen activator inhibitor 1 (PAI-1) that is strong and selective. It has an IC50 value of 157 nM for urokinase plasminogen activator (uPA) and preserves tissue plasminogen activator (tPA) in the presence of PAI-1 [2]. The fluorescence (F1) of fluorophore-labeled PAI-1 (PAI-NBD119) is quenched by PAI-749, which has an IC50 of 140 nM and an apparent Kd of 254 nM[2].
In vitro, PAI-749 preserves tPA activity in the presence of PAI-1 with an IC50 of 154 nM and a Ki of 253 nM. It blocks PAI-1-mediated inhibition of uPA with an IC50 of 87 nM. The compound binds directly to PAI-1 and prevents the formation of the tPA/PAI-1 complex. These properties make PAI-749 a valuable tool for studying fibrinolysis and thrombosis. |
| ln Vivo |
In vivo activity data for PAI-749 are not extensively detailed in the available literature. As a potent PAI-1 antagonist that preserves tPA and uPA activities, the compound would be expected to enhance fibrinolysis and exhibit antithrombotic activity in vivo. It has been studied for its potential in treating cardiovascular diseases.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PAI-749 involve binding assays with purified PAI-1 protein. The compound's ability to bind directly to PAI-1 and block its interaction with tPA is assessed using ELISA or surface plasmon resonance. Inhibition of the tPA/PAI-1 complex formation is measured by gel electrophoresis or chromogenic substrate assays.
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| Cell Assay |
In vitro cell-based assays for PAI-749 use endothelial cells or plasma samples to assess preservation of tPA and uPA activity in the presence of PAI-1. Cells or plasma are treated with PAI-749, and fibrinolytic activity is measured using chromogenic substrates or clot lysis assays. The compound's ability to abrogate PAI-1-mediated inhibition of fibrinolysis is evaluated.
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| Animal Protocol |
In vivo animal studies for PAI-749 have been conducted in models of thrombosis and cardiovascular disease. Animal models such as venous or arterial thrombosis models are used to assess the compound's antithrombotic efficacy. Endpoints include clot formation, thrombus weight, and fibrinolytic activity. The compound's ability to enhance fibrinolysis and prevent thrombus formation is evaluated.
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| ADME/Pharmacokinetics |
PAI-749 (Diaplasinin) has a molecular weight of approximately 468.52 g/mol. The compound is a naphthyl indole-based small molecule. It is supplied as a solid powder and is soluble in DMSO. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PAI-749 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As a PAI-1 antagonist that promotes fibrinolysis, potential toxicities may relate to increased bleeding risk, though formal toxicological profiles are not reported.
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| References |
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| Additional Infomation |
PAI-749 (CAS 481631-45-2), also known as Diaplasinin, is a potent and selective PAI-1 antagonist that preserves tPA and uPA activities. It has an IC50 of 154 nM for tPA preservation and 87 nM for uPA preservation. The compound binds directly to PAI-1 and has antithrombotic activity. No clinical trial or approved indication data are available.
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| Molecular Formula |
C32H31N5O
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|---|---|
| Molecular Weight |
501.63
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| Exact Mass |
501.253
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| CAS # |
481631-45-2
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| PubChem CID |
6450820
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.21g/cm3
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| Boiling Point |
759.2ºC at 760mmHg
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| Flash Point |
413ºC
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| Index of Refraction |
1.661
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| LogP |
7.334
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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 |
10
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| Heavy Atom Count |
38
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| Complexity |
716
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BDPXZFKVHDEPIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H31N5O/c1-2-3-5-13-29-28-12-8-9-14-30(28)37(21-23-10-6-4-7-11-23)32(29)26-16-15-25-20-27(18-17-24(25)19-26)38-22-31-33-35-36-34-31/h4,6-12,14-20H,2-3,5,13,21-22H2,1H3,(H,33,34,35,36)
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| Chemical Name |
1-benzyl-3-pentyl-2-[6-(2H-tetrazol-5-ylmethoxy)naphthalen-2-yl]indole
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| Synonyms |
PAI749; PAI 749; PAI-749
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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 : ~125 mg/mL (~249.19 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 | 1.9935 mL | 9.9675 mL | 19.9350 mL | |
| 5 mM | 0.3987 mL | 1.9935 mL | 3.9870 mL | |
| 10 mM | 0.1994 mL | 0.9968 mL | 1.9935 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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