2. Cytoskeleton Apoptosis
  3. Integrin Apoptosis
  4. BTT-3033

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.

For research use only. We do not sell to patients.

BTT-3033 Chemical Structure

BTT-3033 Chemical Structure

CAS No. : 1259028-99-3

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Customer Review

Based on 1 publication(s) in Google Scholar

BTT-3033 Related Antibodies

Top Publications Citing Use of Products

View All Integrin Isoform Specific Products:

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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Description

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[1][2][4].

IC50 & Target[1][5]

α2β1

130 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
130 nM
Compound: 32
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
[PMID: 31999923]
In Vitro

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 collagenⅠcoated 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.

BTT-3033 Related Antibodies

Cell Viability Assay[4]

Cell Line: LNcap‐FGC, and DU‐145 cells
Concentration: 0.05, 0.5 5, 25, and 50 μM
Incubation Time: 48 h
Result: Decreased the cell viability at 25 μM and 50 μM.

Cell Viability Assay[4]

Cell Line: LNcap‐FGC, and DU‐145 cells
Concentration: 5, 25, and 50 μM
Incubation Time: 48 h
Result: Induced cell apoptosis about 20%, 32%, and 47% (LNcap‐FGC) and 26%, 41%, and 59% (DU‐145) at 5, 25, and 50 μM.

Western Blot Analysis[4]

Cell Line: LNcap‐FGC, and DU‐145 cells
Concentration: 25 μM
Incubation Time: 48 h
Result: Resulted in down-regulation of N‐cadherin and upregulation of E‐cadherin (EMT‐associated proteins).
In Vivo

BTT-3033 (oral administration, 10 mg/kg, at 24 h and 2 h before PAF induction) shows anti-inflammatory effects in mouse air pouch model[2].
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.

Animal Model: PAF (platelet-activating factor)-induced mouse air pouch model[2]
Dosage: 1, 10 mg/kg at 24 h and 2 h before PAF induction
Administration: Oral administration
Result: Reduced the infiltration of leukocytes by about 50% at 10 mg/kg.
Animal Model: Male DBA/1 mice (Pharmacokinetic assay)[2]
Dosage: 10 mg/kg for a single dose
Administration: Oral administration
Result: Plasma levels: about 1 ng/mL at 24 h post-dose.
Molecular Weight

465.50

Formula

C23H20FN5O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1482 mL 10.7411 mL 21.4823 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.22%

SDS (252 KB)

COA (246 KB) HNMR (279 KB) LCMS (102 KB)

Handling Instructions (2659 KB)
References

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
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BTT-3033 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BTT-30331259028-99-3BTT3033BTT 3033IntegrinApoptosisThrombusthrombosisplateletCHO celladhesionear edemaair pouchinflammationsmooth muscle contractionprostateEMTInhibitorinhibitorinhibit

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