| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
S1P1 internalization ( EC50 = 9.83 nM )
YUN88562 targets sphingosine-1-phosphate (S1P) receptors, specifically S1PR4. Activation of S1P receptors modulates immune cell trafficking by regulating lymphocyte egress from lymphoid organs. Through S1PR4 but not S1PR1, S1P blocks the collagen-induced activation of human platelets. This receptor is involved in various physiological processes, including immune cell trafficking, vascular development, and neural function. |
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| ln Vitro |
YUN88562 is a S1P receptor agonist with immunomodulatory activity. It binds to and activates S1P receptors, modulating immune cell trafficking. Through S1PR4 but not S1PR1, it blocks the collagen-induced activation of human platelets. Detailed in vitro potency data are limited, but the compound is active in cellular assays of S1P receptor function.
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| ln Vivo |
Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) exhibits activity at all doses; a 50% reduction in peripheral blood lymphocyte count and a decrease in the 1 mg/kg dose can be observed with a mere 0.01 mg/kg dose. Additionally, the amount of peripheral monocytes and other white blood cells in SD rats is not considerably changed by this compound, which is lymphocyte-specific[1].
Icanbelimod (oral administration; 3 mg/kg; 12 days) is has been demonstrated to prevent lymphocyte outflow. Compound 2 effectively inhibits the development of joint swelling and joint structure destruction in the rat model of type II collagen-induced arthritis[1]. Icanbelimod (oral administration; 0.3-1mg/kg; 30 days; once daily) reduces the risk of experimental autoimmune encephalitis (EAE) in a dose-dependent way in a mouse model[1]. In vivo, YUN88562 (Icanbelimod) exhibits activity at all doses from 0.01 mg/kg to 1 mg/kg when administered orally. A 50% reduction in peripheral blood lymphocyte count is observed with a dose of 0.01 mg/kg. This demonstrates the compound's potent immunomodulatory activity and its ability to modulate lymphocyte trafficking in vivo. |
| Enzyme Assay |
In vitro assays for YUN88562 typically involve measuring its binding to and activation of S1P receptors. Cell lines expressing recombinant S1P receptors are treated with YUN88562, and receptor activation is assessed by measuring downstream signaling pathways, such as GTPγS binding, ERK phosphorylation, or calcium mobilization. EC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for YUN88562 are performed using immune cells, such as lymphocytes or platelets. The compound's effects on lymphocyte migration or platelet activation are assessed. For lymphocyte assays, cells are treated with YUN88562, and their migration in response to S1P gradients is measured using transwell assays. For platelet assays, collagen-induced activation is measured in the presence of YUN88562.
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| Animal Protocol |
Lewis rats
3 mg/kg Oral administration In vivo animal studies with YUN88562 are conducted in mouse models to assess its immunomodulatory effects. Mice are treated with YUN88562 orally at doses ranging from 0.01 mg/kg to 1 mg/kg. Peripheral blood lymphocyte counts are measured, and the compound's effects on lymphocyte trafficking and immune function are assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for YUN88562 are limited. Its molecular weight is approximately 409.18 g/mol. The compound has a molecular formula of C23H24FN3O3. For research use, it is typically dissolved in DMSO for in vitro studies and formulated in suitable vehicles for oral administration in vivo.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for YUN88562 are limited. As an S1P receptor agonist, it may cause immunosuppression and increase the risk of infections. No significant toxicity has been reported in the limited studies available. The compound is intended for laboratory research only and should be handled with standard safety precautions.
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| References | |
| Additional Infomation |
YUN88562 (Icanbelimod) is a research compound developed as an S1P receptor agonist for immunomodulatory applications. It is a potent immunomodulator that reduces peripheral blood lymphocyte counts. The compound is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C23H24FN3O3
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|---|---|
| Molecular Weight |
409.4534
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| Exact Mass |
409.18
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| Elemental Analysis |
C, 67.47; H, 5.91; F, 4.64; N, 10.26; O, 11.72
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| CAS # |
1514888-56-2
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| Related CAS # |
1514888-56-2
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| PubChem CID |
117972004
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| Appearance |
White to off-white solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YBIFMTGYWXNIRZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24FN3O3/c1-14(2)9-15-3-5-16(6-4-15)22-25-21(26-30-22)17-7-8-18(20(24)10-17)11-27-12-19(13-27)23(28)29/h3-8,10,14,19H,9,11-13H2,1-2H3,(H,28,29)
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| Chemical Name |
1-[[2-fluoro-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid
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| Synonyms |
YUN-88562; S1P-agonist-1; DC10392; Icanbelimod; S1p receptor agonist 1; S1p-receptor-agonist-1; YUN88562; YUN 88562
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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: ~6.8 mg/mL (~16.6 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 | 2.4423 mL | 12.2115 mL | 24.4230 mL | |
| 5 mM | 0.4885 mL | 2.4423 mL | 4.8846 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4423 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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