| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Rendomab B4 (0.15–100 nM; overnight–1 hour) binds specifically and with high affinity (apparent Kd* = 0.15 nM) to the human endothelin B receptor expressed on CHO-ETB cells without cross-reactivity with rodent endothelin B receptor or human endothelin A receptor [1]. Rendomab B4 (10 nM; overnight) does not compete with endothelin-1 or endothelin-3 for binding to the human endothelin B receptor on CHO-ETB cells, indicating a different binding site [1]. Rendomab B4 (1 μg/mL; 90 min) recognizes a discontinuous conformational epitope formed by two discontinuous sequences in the N-terminal domain of the human endothelin B receptor, spanning amino acid residues 28–38 and 70–77 [1]. Rendomab B4 (0.14–10 nM; overnight) specifically binds to human endothelin B receptors expressed on various melanoma cell lines, with the highest affinity for UACC-257 cells (apparent Kd = 0.14 nM), and does not bind to endothelin B receptors on non-cancerous HEK293T or HUVEC cells [1]. Rendomab B4 (150 nM; 2 hours 30 minutes) effectively inhibits endothelin-1 and endothelin-3 induced phospholipase C activation in UACC-257 melanoma cells, reducing activity by approximately 75% [1]. Rendomab B4 (150 nM; 2 hours 5 minutes) does not inhibit endothelin-1 or endothelin-3 induced ERK1/2 phosphorylation in UACC-257 melanoma cells, indicating that it has a biased inhibitory effect on the endothelin B receptor signaling pathway [1]. Rendomab B4 (150 nM; 22 h) completely inhibited endothelin-1-induced migration of UACC-257 melanoma cells without affecting basal cell migration [1].
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|---|---|
| ln Vivo |
Rendomab-B49 (chimera xiRB49) (4 mg/kg; intraperitoneal injection; 2 times) did not inhibit the progression of melanoma xenografts in athymic nude mice and no treatment-related toxicities were observed [2].
|
| Cell Assay |
Cell migration assay [1]
Cell Types: UACC-257 human melanoma cells Tested Concentrations: 150 nM (Rendomab B4, pre-incubation); 50 nM ET-1 (stimulation) Incubation Duration: 2 hours (37°C, pre-incubation); 20 hours (37°C, stimulation) Experimental Results: ET-1 completely inhibited the migration of UACC-257 cells, and the migration level was comparable to that of unstimulated cells. In the absence of ET-1, ET-1 had no effect on basal cell migration. Compared with unstimulated cells, ET-1 increased the migration of UACC-257 cells by 3 times. |
| Animal Protocol |
Animal/Disease Models:Athymic nude mice (female, 10 weeks old) [2]
Doses: 4 mg/kg Route of Administration: Intraperitoneal injection; twice administered (days 47 and 80) Experimental Results: No effect on melanoma xenograft progression was observed within 136 days. All mice were euthanized on day 108 due to severe ulceration or excessive tumor size, consistent with the results in the vector control group. No toxic behavior or weight loss was observed. |
| References |
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| Appearance |
Typically exists as solids at room temperature
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|---|---|
| SMILES |
[Rendomab B4]
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| Synonyms |
Rendomab-B49
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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.
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