G-744 is a highly potent, selective for Btk inhibitor. G-774 is metabolically stable, well tolerated, and efficacious in an animal model of arthritis. G-744 prevents cellular functions in murine B-cells such as B-cell receptor (BCR)-mediated CD86 induction with an EC50 of 64nM. G-744 also inhibited BCR-stimulated B-cell proliferation in human B-cells (EC50 = 22 nM). In human monocytes, production of the inflammatory cytokine TNFα following activation with immune complexes was abrogated by G-744 (EC50 = 33 nM). In human whole blood, G-744 demonstrated potent inhibition of BCR-stimulated CD69 expression on Bcells with an EC50 of 87 nM.
MedKoo Cat#: 530642
Name: G-744
CAS#: 1346669-54-2
Chemical Formula: C29H29N5O3S
Exact Mass: 527.1991
Molecular Weight: 527.64
Elemental Analysis: C, 66.01; H, 5.54; N, 13.27; O, 9.10; S, 6.08
The following data is based on the product molecular weight 527.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
