SB-273005
Based on 1 Customer Validation
SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .
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- Pureté: 99.94%
- CAS No.: 205678-31-5
- Formule: C22H24F3N3O4
- Masse moléculaire:451.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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IL-10 |
αvβ3 1.2 nM (Ki) |
αvβ5 0.3 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.15 nM
Compound: 8
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Inhibition of Vitronectin receptor, integrin alphaV-beta3 expressed in HEK 293 cells
Inhibition of Vitronectin receptor, integrin alphaV-beta3 expressed in HEK 293 cells
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[PMID: 12477347] |
| HEK293 | IC50 |
3 nM
Compound: 7
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HEK cell adhesion mediated by alpha v beta 3 integrin
HEK cell adhesion mediated by alpha v beta 3 integrin
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[PMID: 10633035] |
SB-273005 (0.1 nM-1 µM; 1 h) dose-dependently inhibits adhesion of mouse and monkey VSMCs to vitronectin-coated plates, with similar IC50 values (2.9 nM for mouse, 6.9 nM for monkey)[2].
SB-273005 (100 nM-100 µM) inhibits TGFβ-induced Rictor phosphorylation and VSMC migration in mouse aortic smooth muscle cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SB-273005 (300-1000 mg/kg; p.o.; daily; 3-14 days) causes acute aortic and renal artery smooth muscle cell necrosis, followed by medial hypertrophy and fibrosis in CD-1 mice[2].
SB-273005 (3 mg/kg; p.o.; during days 3-5 of pregnancy) reduces splenic Th2 cell polarization and IL-10 secretion, reversing pregnancy-induced immune deviation in pregnant mice[4].
SB-273005 (3-30 mg/kg; p.o.; once daily; 8 days) decreases urinary deoxypyridinoline (bone resorption marker) and preserves trabecular bone density in Thyroxine-induced osteopenic rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Lewis rats (6-8 weeks, 160-180 g), adjuvant-induced arthritis (AIA)[1]
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Dosage:10, 30, 60 mg/kg
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Administration:Oral gavage (p.o.), twice daily (prophylactic: days 0-20; therapeutic: days 10-20)
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Result:Reduced paw edema by 40-52% (prophylactic) and 36-48% (therapeutic), with significant preservation of bone mineral density (BMD) and joint structure via DEXA, MRI, and histology.
Chemical Information
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CAS No. 205678-31-5
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Appearance Solid
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Masse moléculaire 451.44
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Formule C22H24F3N3O4
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Color White to off-white
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SMILES
O=C(O)C[C@H]1C(N(CC(F)(F)F)CC2=CC(OCCC3=NC(NC)=CC=C3)=CC=C2C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (221.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Badger AM, et al. Disease-modifying activity of SB 273005, an orally active, nonpeptide alphavbeta3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthritis. Arthritis Rheum. 2001 Jan;44(1):128-37. [Content Brief]
[2]. Rehm S, et al. Novel vascular lesions in mice given a non-peptide vitronectin receptor antagonist. Toxicol Pathol. 2007 Dec;35(7):958-71. [Content Brief]
[3]. Parker SJ, et al. Proteomics reveals Rictor as a noncanonical TGF-β signaling target during aneurysm progression in Marfan mice. Am J Physiol Heart Circ Physiol. 2018 Nov 1;315(5):H1112-H1126. [Content Brief]
[4]. Wang S, et al. SB-273005, an antagonist of αvβ3 integrin, reduces the production of Th2 cells and cytokine IL-10 in pregnant mice. Exp Ther Med. 2014 Jun;7(6):1677-1682. [Content Brief]
[5]. Hoffman SJ, et al. Rapid inhibition of thyroxine-induced bone resorption in the rat by an orally active vitronectin receptor antagonist. J Pharmacol Exp Ther. 2002 Jul;302(1):205-11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2151 mL | 11.0757 mL | 22.1513 mL | 55.3783 mL |
| 5 mM | 0.4430 mL | 2.2151 mL | 4.4303 mL | 11.0757 mL | |
| 10 mM | 0.2215 mL | 1.1076 mL | 2.2151 mL | 5.5378 mL | |
| 15 mM | 0.1477 mL | 0.7384 mL | 1.4768 mL | 3.6919 mL | |
| 20 mM | 0.1108 mL | 0.5538 mL | 1.1076 mL | 2.7689 mL | |
| 25 mM | 0.0886 mL | 0.4430 mL | 0.8861 mL | 2.2151 mL | |
| 30 mM | 0.0738 mL | 0.3692 mL | 0.7384 mL | 1.8459 mL | |
| 40 mM | 0.0554 mL | 0.2769 mL | 0.5538 mL | 1.3845 mL | |
| 50 mM | 0.0443 mL | 0.2215 mL | 0.4430 mL | 1.1076 mL | |
| 60 mM | 0.0369 mL | 0.1846 mL | 0.3692 mL | 0.9230 mL | |
| 80 mM | 0.0277 mL | 0.1384 mL | 0.2769 mL | 0.6922 mL | |
| 100 mM | 0.0222 mL | 0.1108 mL | 0.2215 mL | 0.5538 mL |
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