An integrin α2β1 inhibitor
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BTT3033

Item No. 42119

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-fluorophenyl)-N-methyl-N-[4-[[(phenylamino)carbonyl]amino]phenyl]-1H-pyrazole-4-sulfonamide
CAS Number
1259028-99-3
Molecular Formula
C23H20FN5O3S
Formula Weight
465.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=S(C1=CN(C2=CC=C(F)C=C2)N=C1)(N(C3=CC=C(NC(NC4=CC=CC=C4)=O)C=C3)C)=O
InChi Code
InChI=1S/C23H20FN5O3S/c1-28(33(31,32)22-15-25-29(16-22)21-11-7-17(24)8-12-21)20-13-9-19(10-14-20)27-23(30)26-18-5-3-2-4-6-18/h2-16H,1H3,(H2,26,27,30)
InChi Key
NSLIQOPYDUKWTA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Cayman Chemical
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    Product Description

    BTT3033 is an inhibitor of integrin α2β1 (EC50 = 130 nM in CHO cells expressing the human receptor).1 It is 8-fold selective for integrin α2β1 over integrin α1β1, as well as laminin 332, 40 kDa fibronectin, 120 kDa fibronectin, and vitronectin at 130 nM. BTT3033 inhibits the adhesion of platelets in isolated mouse whole blood to collagen I-coated capillaries at a constant shear rate (EC50 = 6 µM). In vivo, BTT3033 (10 mg/kg, p.o.) decreases lavage fluid leukocyte infiltration in a mouse model of platelet-activating factor-induced air pouch inflammation.2 It decreases ear thickness in a mouse model of ovalbumin- and alum-induced mouse model of skin hypersensitivity when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nissinen, L., Koivunen, J., Käpylä, J., et al. Novel α2β1 integrin inhibitors reveal that integrin binding to collagen under shear stress conditions does not require receptor preactivation. The Journal of Biological Chemisty 287(53), 44694-44702 (2012).

    2. Nissinen, L., Ojala, M., Langen, B., et al. Sulfonamide inhibitors of α2β1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation. Pharmacol. Res. Perspect. 3(3), e00146 (2015).