| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In HEK293 cells, SB 452533 has a strong antagonistic effect on the cloned recombinant rat TRPV1 receptor, with a pKb of 7.7 and a pIC50 of 7.0 [1]. AMPK and CAMKK2 phosphorylation is decreased by SB-452533 [2].
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|---|---|
| ln Vivo |
SB-452533 reverses the effects of small doses of capsaicin (Cap; low dose 2 mg/kg) and greatly reduces bleomycin-induced lung fibrosis in mice [3].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Skeletal Muscle (C2C12) Cell Tested Concentrations: 0, 50, 100, 200 and 400 μM Incubation Duration: 30 minutes; then treated with 200 μM capsaicin for an additional 30 minutes. Experimental Results: Dramatically diminished capsaicin-induced AMPK and CAMKK2 phosphorylation. |
| Animal Protocol |
Animal/Disease Models: BALB/c mouse pulmonary fibrosis model [3]
Doses: 2.5 mg/kg Route of Administration: Daily subcutaneous injection for 21 days Experimental Results: Effect of Cap (reduce bleomycin-induced pulmonary fibrosis ) in the presence of SB-452533. |
| References |
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| Exact Mass |
375.095
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|---|---|
| CAS # |
459429-39-1
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| PubChem CID |
9842609
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| Appearance |
White to off-white solid powder
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| LogP |
4.682
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
366
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CCNC(=O)NC1=CC=CC=C1Br)C2=CC=CC(=C2)C
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| InChi Key |
IFJYEGJUQIBBQV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22BrN3O/c1-3-22(15-8-6-7-14(2)13-15)12-11-20-18(23)21-17-10-5-4-9-16(17)19/h4-10,13H,3,11-12H2,1-2H3,(H2,20,21,23)
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| Chemical Name |
1-(2-bromophenyl)-3-[2-(N-ethyl-3-methylanilino)ethyl]urea
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| Synonyms |
SB452533 SB-452533 SB 452533
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~265.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.64 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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