| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
EC50: 398 nM (S1PR1)[1].
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| ln Vitro |
W146 is an antagonist of S1PR1 with a Ki of roughly 70–80 nM[1]. The W146 pretreatment markedly raised the amounts of activated cleaved caspase-3. The S1P-induced decrease in EPC apoptosis totally vanished following W146 therapy [2].
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| ln Vivo |
Pretreatment with W146 (5 mg/kg, ip) prior to AMD3100 administration resulted in an approximately 8-fold increase in KSL-HSPC mobilization as compared to mice treated with AMD3100 alone, as shown by the CFU-G/M colony formation assay [3]. The particular augmentation of KSL-HSPC mobilization by W146 was mediated, since pretreatment of mice with W140 did not affect the activation of AMD3100-stimulated KSL-HSPC. Mice's basal WBC counts remain unchanged after injections of W146, W140, JTE013 or Cay10444 [3].
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| Cell Assay |
Apoptosis Analysis[2]
Cell Types: Endothelial progenitor cells (EPCs). Tested Concentrations: 10 μM. Incubation Duration: 30 min before the addition of S1P. Experimental Results: Increases activated cleaved caspase-3 levels. |
| Animal Protocol |
Animal/Disease Models: Mice (4-6weeks old)[3] .
Doses: 5 mg/kg. Route of Administration: IP, 1 hour prior to AMD3100 (ADM) administration. Experimental Results: Dramatically increased in KSL-HSPC mobilization compared to that in mice pretreated with dextran followed by AMD3100 administration. |
| References |
[1]. M Germana Sanna, et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2006 Aug;2(8):434-41. Epub 2006 Jul 9.
[2]. Jingjing Liu, et al. 3-amino-4-(3-hexylphenylamino)-4-oxobutyl phosphonic acid (W146), a Selective Antagonist of Sphingosine-1-phospahte Receptor Subtype 1, Enhances AMD3100-stimulated Mobilization of Hematopoietic Stem Progenitor Cells in Animals. J Biochem Pharmacol Res. 2013 Dec; 1(4): 197–203. [3]. Hang Wang, et al. Sphingosine-1-phosphate promotes the proliferation and attenuates apoptosis of Endothelial progenitor cells via S1PR1/S1PR3/PI3K/Akt pathway. Cell Biol Int. 2018 May 23. |
| Molecular Formula |
C18H28F3N2O6P
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|---|---|
| Molecular Weight |
456.39
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| CAS # |
909725-62-8
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| Related CAS # |
W146;909725-61-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
P(CCC(C(NC1=CC=CC(=C1)CCCCCC)=O)N)(=O)(O)O.FC(C(=O)O)(F)F
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : 22.73 mg/mL (49.80 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 | 2.1911 mL | 10.9555 mL | 21.9111 mL | |
| 5 mM | 0.4382 mL | 2.1911 mL | 4.3822 mL | |
| 10 mM | 0.2191 mL | 1.0956 mL | 2.1911 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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