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ln Vitro |
For the recombinant SIGLEC8 extracellular domain (ECD), the antigen-binding fragment (fab) of lerentelimab has an affinity of 464 pM [1]. When produced in vitro, on eosinophils, and on NK cells that express SIGLEC8 through its Fc domain in human blood, lidentelimab exhibits a strong affinity for these cell types [1]. Human peripheral blood eosinophils and human lung tissue eosinophils and mast cells are specifically bound by lientrelimab (1 µg/mL) [1]. Inducing apoptosis in IL-5-activated eosinophils, lidentelimab (0.0001-100 μg/mL; 30 min) [1]. Immunodestructive cellular cytotoxicity (ADCC) is produced by lidentelimab (30 min), which has an EC50 of 1.9 ng/mL on eosinophils in peripheral blood leukocyte (PBL) preparations from healthy volunteers [1]. The amount of eosinophils in separated human tissue is decreased by lidentelimab [1].
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ln Vivo |
In a mouse model of systemic allergic reaction, lidentelimab (100 μg; intravenous injection, once) effectively suppresses IgE-mediated mast cell activation [1].
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Cell Assay |
Apoptosis Analysis[1]
Cell Types: Eosinophils Tested Concentrations: 10 μg/mL-1 pg/mL Incubation Duration: 30 min Experimental Results: Dose- dependently induced apoptosis of IL-5-activated (50 ng/mL) eosinophils. |
Animal Protocol |
Animal/Disease Models: Humanized mice (NSG-SGM3) engrafts with human thymus, liver, and HSC[1]
Doses: 100 μg Route of Administration: intravenous (iv)injection; 100 μg , once Experimental Results: Completely prevented passive systemic anaphylaxis (PSA) as shown by a lack of change in rectal temperature and symptom scores in mice. |
References |
[1]. Youngblood BA, et al. AK002, a Humanized Sialic Acid-Binding Immunoglobulin-Like Lectin-8 Antibody that Induces Antibody-Dependent Cell-Mediated Cytotoxicity against Human Eosinophils and Inhibits Mast Cell-Mediated Anaphylaxis in Mice. Int Arch Allergy Immunol. 2019;180(2):91-102.
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CAS # |
2283348-97-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
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
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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.) |
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.