SB-505124 hydrate hydrochloride
SB505124
CAS: 694433-59-5
Molecular Formula: C20H21N3O2
SB-505124 hydrate hydrochloride - Names and Identifiers
SB-505124 hydrate hydrochloride - Physico-chemical Properties
| Molecular Formula | C20H21N3O2 |
| Molar Mass | 335.4 |
| Density | 1.202 |
| Melting Point | 168 °C |
| Boling Point | 509.7±50.0 °C(Predicted) |
| Solubility | DMSO: >10mg/mL |
| Appearance | powder |
| Color | yellow |
| pKa | 11.26±0.10(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| Use | SB505124 is a selective TGF βR inhibitor that acts on ALK4 and ALK5. IC50 is 129 nM and 47 nM respectively in cell-free test. It also inhibits ALK7 but not ALK1,2,3 or 6. |
| In vitro study | SB-505124 inhibition of the closely related ALK4 with an IC50 of 129 nM was 2.5-fold less selective than for alk5. ALK2 was also not inhibited at SB-505124 concentrations up to 10 μm. SB-505124 acts on COS-1 cells and also inhibits endogenous Smad2 phosphorylation. The addition of SB-505124 does not affect the constitutively active ALK1, ALK2, ALK3, and ALK6 phosphorylation of smad1. ALK4 and ALK5 activate Smad1 and Smad2, and the addition of SB-505124 inhibits activation. SB-505124 inhibits Smad2 phosphorylation induced by TGF-β in HepG2 human hepatoma cells, C2C12 mouse myoblasts and Mv1Lu mink lung cells in a concentration-dependent manner. 1 μm SB-505124 also inhibited Activin-induced Smad2 phosphorylation. SB-505124 potent inhibition of TGF-β and Activin-induced caga12-luciferase and ARE-luciferase receptor structures in a concentration-dependent manner. SB-505124 can eliminate the inhibition of E-cadherin promoter, mRNA and protein expression by TGF-β1. SB-505124 impaired Smad2 phosphorylation and expression of CTGF and alpha-SMA. |
| In vivo study | SB-505124 treated filtering blebs in glaucoma filtration surgery for more than 10 days without any serious post-operative complications, and follicles were clearly observed. The intraocular pressure (IOP) was less than 10 mm Hg in the first week, whereas the IOP rose to 10 mm Hg after one week of SB-505124 treatment. |
SB-505124 hydrate hydrochloride - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
| HS Code | 29349990 |
SB-505124 hydrate hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.982 ml | 14.908 ml | 29.815 ml |
| 5 mM | 0.596 ml | 2.982 ml | 5.963 ml |
| 10 mM | 0.298 ml | 1.491 ml | 2.982 ml |
| 5 mM | 0.06 ml | 0.298 ml | 0.596 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: SB505124 Visit Supplier Webpage Request for quotationCAS: 694433-59-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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