| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
NP-313 targets multiple pathways: it inhibits thromboxane A₂ synthase (TXA2 synthase), reducing TXA2 production; it selectively inhibits store-operated calcium channel (SOCC)-mediated Ca²⁺ influx; and it binds to the SRA domain of UHRF1, a protein involved in DNA methylation and epigenetic regulation. At 10 µM, NP-313 also inhibits cyclooxygenase (COX) and protein kinase C (PKC).
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| ln Vitro |
In a dose-dependent manner, NP-313 (0-80 μM) suppresses static aggregase. For example, NP-313 can inhibit port- and A23187-induced static aggregation to a maximum degree of 80% and 60%, respectively [1 NP-313 (0-8 μM) concentration inhibits P-selectin expression and collagen in a suspended manner or activates enzyme-induced thromboxane B 2 (TXB2) production in humans. NP-313 also inhibits COX– at the same time. For TXA 2 synthase, the IC 50 values are 3.9 µM and 1.5 µM, respectively[1].
In vitro, NP-313 (0-80 μM) inhibits platelet aggregation in a dose-dependent manner, reducing thrombin- and A23187-induced aggregation. It inhibits thromboxane A₂ synthesis and SOCC-mediated Ca²⁺ influx. In FRET assays, NP-313 inhibits binding of UHRF1 to hemi-methylated DNA with IC50 of 499.4 nM and binds to the SRA domain with KD of 3.71 μM. These activities demonstrate its potential as both an antithrombotic and an epigenetic modulator. |
| ln Vivo |
Time to occlusion (TTO), buffering time, and ring aggregation induced by collagen (10 µg/mL) are all markedly prolonged in kit ICR by NP-313 (iv, 4–16 µg/g) [1].
In vivo, NP-313 functions as a potent antithrombotic agent that inhibits platelet aggregation and activation. By inhibiting TXA2 synthesis and SOCC-mediated calcium influx, it reduces thrombus formation in animal models of thrombosis. Its additional inhibition of COX and PKC may contribute to its antiplatelet effects. However, detailed in vivo efficacy data in specific thrombosis models is limited in publicly available sources. |
| Enzyme Assay |
In vitro enzyme assays for NP-313 measure inhibition of thromboxane A₂ synthase activity using radiolabeled substrates or ELISA-based TXB2 (stable metabolite of TXA2) quantification. Cyclooxygenase (COX) activity is assessed by measuring prostaglandin production. Protein kinase C (PKC) activity is measured using kinase assays with peptide substrates. For UHRF1 binding, FRET-based assays or surface plasmon resonance (SPR) are used to measure binding affinity to the SRA domain.
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| Cell Assay |
Cellular assays for NP-313 use human or rodent platelets. Platelets are isolated from whole blood and treated with NP-313 at various concentrations (0-80 μM). Platelet aggregation is induced by agonists such as thrombin or A23187, and aggregation is measured using a platelet aggregometer. Thromboxane B2 levels in platelet supernatants are measured by ELISA to confirm TXA2 synthase inhibition. Calcium flux is measured using fluorescent calcium indicators (e.g., Fluo-4) to assess SOCC inhibition.
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| Animal Protocol |
In vivo animal studies for NP-313 typically utilize rodent models of thrombosis, such as ferric chloride-induced arterial thrombosis or pulmonary embolism models. The compound is administered intravenously or intraperitoneally. Endpoints include time to occlusion, thrombus weight, bleeding time, and platelet count. Efficacy is compared to vehicle and reference antiplatelet agents (e.g., aspirin, clopidogrel). Tolerability and bleeding risk are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NP-313 are not extensively documented. As a small molecule with molecular weight of approximately 287.7 g/mol (C₁₅H₁₀ClNO₃), it is expected to have moderate oral bioavailability. It is soluble in DMSO. Detailed PK parameters (half-life, Cmax, AUC, clearance) would need to be determined in preclinical species to support in vivo efficacy studies. The compound's multiple targets suggest a complex pharmacodynamic profile.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of NP-313 is not extensively documented in publicly available sources. As an antithrombotic agent, the primary safety concern is bleeding risk due to inhibition of platelet function and TXA2 synthesis. Standard toxicology studies would evaluate bleeding time, platelet count, and coagulation parameters. Additional studies would assess potential off-target effects on COX and PKC pathways. Maximum tolerated dose would be determined in rodent models.
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| References | |
| Additional Infomation |
NP-313 is a specific small molecule ubiquitin-like protein UHRF1 inhibitor that binds to the SRA domain groove of UHRF1.
NP-313 (NSC-4264, UF146) is a potent antithrombotic agent with dual inhibition of TXA2 synthesis and SOCC-mediated Ca²⁺ influx. It also binds UHRF1 and inhibits its interaction with hemi-methylated DNA. It inhibits COX and PKC at higher concentrations. It is available for research purposes only and is not approved for clinical use. |
| Molecular Formula |
C12H8CLNO3
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|---|---|
| Molecular Weight |
249.65
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| Exact Mass |
249.019
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| CAS # |
5397-78-4
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| PubChem CID |
72754
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.44g/cm3
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| Boiling Point |
427.7ºC at 760 mmHg
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| Flash Point |
212.5ºC
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| Index of Refraction |
1.62
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| LogP |
2.043
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OMXMYDUYAUOFRX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H8ClNO3/c1-6(15)14-10-9(13)11(16)7-4-2-3-5-8(7)12(10)17/h2-5H,1H3,(H,14,15)
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| Chemical Name |
N-(3-chloro-1,4-dioxonaphthalen-2-yl)acetamide
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| Synonyms |
NP313; NP 313; NP-313
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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 : ~25 mg/mL (~100.14 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 | 4.0056 mL | 20.0280 mL | 40.0561 mL | |
| 5 mM | 0.8011 mL | 4.0056 mL | 8.0112 mL | |
| 10 mM | 0.4006 mL | 2.0028 mL | 4.0056 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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