| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:G-744
CAS:1346669-54-2
Package:100mg/RMB 39500;50mg/RMB 30300;25mg/RMB 22700
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| Product Name: | G-744 | | Synonyms: | G-744;G744,G 744;2H-Cyclopenta[4,5]thieno[2,3-c]pyridin-1(5H)-one, 2-[3-[1,6-dihydro-1-methyl-6-oxo-5-(4-pyrimidinylamino)-3-pyridinyl]-2-(hydroxymethyl)phenyl]-3,4,6,7-tetrahydro-6,6-dimethyl- | | CAS: | 1346669-54-2 | | MF: | C29H29N5O3S | | MW: | 527.64 | | EINECS: | | | Product Categories: | | | Mol File: | 1346669-54-2.mol |  |
| | G-744 Chemical Properties |
| Boiling point | 820.6±65.0 °C(Predicted) | | density | 1.382±0.06 g/cm3(Predicted) | | pka | 13.99±0.10(Predicted) |
| | G-744 Usage And Synthesis |
| Description | 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. | | Uses | G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis[1]. | | in vivo | G-744 (6.25/12.25/25 mg/kg, p.o., b.i.d., daily) protects Lewis rats from collagen-induced arthritis dose-dependently[1]. | Animal Model: | Female Lewis rat based CIA models[1]. | | Dosage: | 6.25, 12.25, 25 mg/kg. | | Administration: | Orally, b.i.d., daily for 17 days. | | Result: | All three doses resulted in a significant dose-dependent inhibition of ankle thickness between day 10 and day 17 (onset of increase in ankle diameter on day 9). |
| | References | [1] Wang X, et al. Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties. ACS Med Chem Lett. 2017 May 3;8(6):608-613. DOI:10.1021/acsmedchemlett.7b00103 |
| | G-744 Preparation Products And Raw materials |
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