| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PI3K-001 (50 μM; incubated at 37 °C for 30 minutes) showed a binding rate of over 97% to albumin in both human and mouse plasma[1]. PI3K-001 (50 μM; incubated at 37 °C for 1–7 days) exhibited high plasma stability, with the release of its active payload P001 being less than 1% after 7 days of incubation at 37 °C in both human and mouse plasma[1].
|
|---|---|
| ln Vivo |
PI3K-001 (9.5 mg/kg; intravenous injection; single dose) can target and deliver P001 to fibrotic lung tissue and maintain the drug in the lung tissue for at least 18 hours [1]. PI3K-001 (25 mg/kg; intravenous injection; once every 7 days; for a total of 2 doses) showed superior anti-fibrotic efficacy in a bleomycin-induced mouse pulmonary fibrosis model, significantly improving survival, reducing weight loss and lowering the levels of pulmonary fibrosis markers compared to the parent drug P001 [1]. PI3K-001 (3 mg/kg; intravenous injection; single dose) showed superior pharmacokinetic properties in healthy SD rats, with Cmax and AUC being 10-fold and 7-fold higher than the parent drug P001, respectively, indicating increased systemic exposure and prolonged circulation time [1].
|
| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, 20-22 g, bleomycin-induced pulmonary fibrosis) [1]
Doses: 9.5 mg/kg Route of Administration: Intravenous injection; single dose Experimental Results: Six hours after administration, the concentration of P001 in lung tissue was significantly higher than that in the maternal P001 group. Eighteen hours after administration, the concentration of P001 in lung tissue was still detectable, reaching a maximum of approximately 50 ng/g, while P001 was almost undetectable in lung tissue. Animal/Disease Models:C57BL/6 (male, bleomycin-induced pulmonary fibrosis)[1] Doses: 25 mg/kg Route of Administration: Intravenous injection; once every 7 days; for a total of 2 doses Experimental Results: The survival rate of mice was significantly improved compared with the P001 group. Weight loss was reduced compared with the P001 group. The increase in bleomycin-induced lung weight and lung index was significantly reduced, and the improvement was better than that of the P001 group and the positive control nintedanib. Lung collagen deposition was significantly reduced, and alveolar structure was maintained. Masson staining and H&E staining showed that the lung tissue morphology was closer to normal than that of the P001 group. |
| References |
| Molecular Formula |
C82H111F2N11O22S2
|
|---|---|
| Molecular Weight |
1704.95
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COC1=C(C=C(C=N1)C2=CC3=C(N=CC=C3C4=CN=C(C=C4)COCN(C(OCC5=CC=C(C=C5)NC([C@@H](NC([C@H](C(C)C)NC(COCCOCCNC(COCCOCCNC(CC[C@@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)C)=O)=O)CCS(C)(=O)=O)C=C2)NS(=O)(C6=CC=C(C=C6F)F)=O
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 0.5865 mL | 2.9326 mL | 5.8653 mL | |
| 5 mM | 0.1173 mL | 0.5865 mL | 1.1731 mL | |
| 10 mM | 0.0587 mL | 0.2933 mL | 0.5865 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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