G-744
- CAS No.
- 1346669-54-2
- Chemical 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-
- CBNumber:
- CB64667922
- Molecular Formula:
- C29H29N5O3S
- Molecular Weight:
- 527.64
- MDL Number:
- MFCD31556562
- MOL File:
- 1346669-54-2.mol
- MSDS File:
- SDS
- TDS File:
- TDS
G-744 Chemical Properties, Uses, Production
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
Raw materials
Preparation Products
G-744 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6288 | 58 |
| Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 11975 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9831 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29873 | 58 |
