BTT-3033
Based on 1 publication(s) in Google Scholar
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease.
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- Pureza: 96.57%
- No. CAS: 1259028-99-3
- Fòrmula: C23H20FN5O3S
- Peso molecular:465.50
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Apoptosis Compound Library
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) BTT-3033
More
Actividad biológica
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α2β1 130 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
130 nM
Compound: 32
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Inhibition of human alpha2 beta1 expressed in CHO cells assessed as reduction in cell adhesion to collagen type 1 incubated for 5 mins by DiOC6 dye based fluorescence microscopy
Inhibition of human alpha2 beta1 expressed in CHO cells assessed as reduction in cell adhesion to collagen type 1 incubated for 5 mins by DiOC6 dye based fluorescence microscopy
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[PMID: 31999923] |
BTT-3033 (1 nM-100 μM, 2 h) inhibits CHO-α2wt cell adhesion to rat tail collagen I (EC50: 130 nM), exhibits selectivity for α2β1 over α3β1, α4β1, α5β1 and αv[1].
BTT-3033 (10 μM, 5 min) inhibits human platelet binding to collagen I coated capillaries under flow, with the EC50 value for mouse whole blood to be 6 μM[1].
BTT-3033 (10 μM, 5 min) inhibits binding of α2-expressing CHO cells to collagen I under shear stress conditions[1].
BTT-3033 (1 μM, 60 min) inhibits of neurogenic and thromboxane A2-induced human prostate smooth muscle contraction[3].
BTT-3033 (25 and 50 μM, 48 h) inhibits cell viability and proliferation by inducing G1 cell cycle arrest in LNcap-FGC, and DU-145 cells[4].
BTT-3033 (50 μM, 48 h) induces apoptosis through the activation of ROS, Bax protein upregulation, caspase-3 activation, and depletion of ΔΨm[4].
BTT-3033 (10 μM, 15/28 days) suppresses MMP13 expression, increases the expression of MMP1 and MT-MMP1 in human articular cartilage derived chondrocytes[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNcap-FGC, and DU-145 cells
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Concentration:0.05, 0.5 5, 25, and 50 μM
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Incubation Time:48 h
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Result:Decreased the cell viability at 25 μM and 50 μM.
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Cell Line:LNcap-FGC, and DU-145 cells
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Concentration:5, 25, and 50 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis about 20%, 32%, and 47% (LNcap-FGC) and 26%, 41%, and 59% (DU-145) at 5, 25, and 50 μM.
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Cell Line:LNcap-FGC, and DU-145 cells
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Concentration:25 μM
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Incubation Time:48 h
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Result:Resulted in down-regulation of N-cadherin and upregulation of E-cadherin (EMT-associated proteins).
BTT-3033 (oral administration, 10 mg/kg, at 48 ,24 and 2 h before ear swelling) shows anti-inflammatory effects in arachidonic acid-induced ear edema model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PAF (platelet-activating factor)-induced mouse air pouch model[2]
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Dosage:1, 10 mg/kg at 24 h and 2 h before PAF induction
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Administration:Oral administration
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Result:Reduced the infiltration of leukocytes by about 50% at 10 mg/kg.
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Animal Model:Male DBA/1 mice (Pharmacokinetic assay)[2]
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Dosage:10 mg/kg for a single dose
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Administration:Oral administration
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Result:Plasma levels: about 1 ng/mL at 24 h post-dose.
Chemical Information
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No. CAS 1259028-99-3
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Appearance Solid
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Peso molecular 465.50
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Fòrmula C23H20FN5O3S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(N(S(=O)(C2=CN(C3=CC=C(C=C3)F)N=C2)=O)C)C=C1)NC4=CC=CC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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FASEB J
Adipocyte Deficiency Promotes Early Development of Mammary Gland Alveolar Epithelial Cell. [Abstract]2025 Nov 15;39(21):e71219. PMID: 41186192
Solvente y solubilidad
DMSO : 250 mg/mL (537.06 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)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liisa Nissinen, et al. Novel α2β1 integrin inhibitors reveal that integrin binding to collagen under shear stress conditions does not require receptor preactivation. J Biol Chem. 2012 Dec 28;287(53):44694-702. [Content Brief]
[2]. Liisa Nissinen, et al. Sulfonamide inhibitors of α2β1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation. Pharmacol Res Perspect. 2015 Jun;3(3):e00146. [Content Brief]
[3]. Bingsheng Li, et al. Inhibition of neurogenic and thromboxane A 2 -induced human prostate smooth muscle contraction by the integrin α2β1 inhibitor BTT-3033 and the integrin-linked kinase inhibitor Cpd22. Prostate. 2020 Aug;80(11):831-849. [Content Brief]
[4]. Zahra Salemi, et al. Integrin α2β1 inhibition attenuates prostate cancer cell proliferation by cell cycle arrest, promoting apoptosis and reducing epithelial-mesenchymal transition. J Cell Physiol. 2021 Jul;236(7):4954-4965. [Content Brief]
[5]. Takashi Kanamoto, et al. Integrin α2β1 plays an important role in the interaction between human articular cartilage-derived chondrocytes and atelocollagen gel. Sci Rep. 2021 Jan 19;11(1):1757. [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 | 2.1482 mL | 10.7411 mL | 21.4823 mL | 53.7057 mL |
| 5 mM | 0.4296 mL | 2.1482 mL | 4.2965 mL | 10.7411 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1482 mL | 5.3706 mL | |
| 15 mM | 0.1432 mL | 0.7161 mL | 1.4322 mL | 3.5804 mL | |
| 20 mM | 0.1074 mL | 0.5371 mL | 1.0741 mL | 2.6853 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8593 mL | 2.1482 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7161 mL | 1.7902 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5371 mL | 1.3426 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0741 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5371 mL |
BTT-3033 Related Classifications
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