HS-276 manufacturers
- HS-276
-
- $37.00
-
2026-07-27
- CAS:2767422-72-8
- Purity: 97.67%
- Supply Ability: 10g
|
| Product Name: | HS-276 | | Synonyms: | HS-276;1,3-Benzenedicarboxamide, N1-[6-(1-piperidinylmethyl)-1-propyl-1H-benzimidazol-2-yl]-;N-(6-(Piperidin-1-ylmethyl)-1-propyl-1H-benzo[d]imidazol-2-yl)isophthalamide;HS-276, 10 mM in DMSO;HS-276 ,E1155 | | CAS: | 2767422-72-8 | | MF: | C24H29N5O2 | | MW: | 419.52 | | EINECS: | | | Product Categories: | | | Mol File: | 2767422-72-8.mol |  |
| | HS-276 Chemical Properties |
| density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (119.18 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 80°C) | | pka | 12.32±0.43(Predicted) | | form | Solid | | color | Off-white to light yellow | | InChIKey | NPEMHKSMWPZEOV-UHFFFAOYSA-N | | SMILES | O=C(C1=CC=CC(C(NC2=NC3=C(N2CCC)C=C(CN4CCCCC4)C=C3)=O)=C1)N |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | HS-276 Usage And Synthesis |
| Uses | HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research[1]. | | Biological Activity | HS-276 is an orally active, potent and selective TGF-β-activated kinase-1 (TAK-1; TAK1) inhibitor (Ki = 2.5 nM; IC50 = 8.25 nM) th at significantly reduced cytokines production in THP-1 human macrophages upon LPS/IFNγ treatment (IC50 = 138 nM/TNF, 201 nM/IL-6, and 234 nM/IL-1β). HS-276 effectively attenuates arthritic-like symptoms in the CIA mouse rheumatoid arthritis (RA) model (10-30 mg/kg/d p.o. or 25 mg/kg/d i.p.). | | in vivo | HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) reduces inflammation, pannus, cartilage damage (CD), bone resorption (BR), and periosteal bone formation (PBF) histological manifestations[1].
HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a Cmax of 3.68 μM and %F of 98.1%[1]. | | IC 50 | IRAK1: 264 nM (IC50); IRAK4: 2500 nM (IC50) | | References | [1] Scarneo S, et al. Development and Efficacy of an Orally Bioavailable Selective TAK1 Inhibitor for the Treatment of Inflammatory Arthritis. ACS Chem Biol. 2022 Mar 18;17(3):536-544. DOI:10.1021/acschembio.1c00788 |
| | HS-276 Preparation Products And Raw materials |
|