| Company Name: |
Wuhan Acumen Bio-Technology Co.,ltd Gold
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| Tel: |
027-027-16602739303 16602739303 |
| Email: |
673003916@qq.com |
| Products Intro: |
Product Name:YQ128
CAS:2454246-18-3
Purity:95%,98% Package:5G
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| Product Name: | YQ128 | | Synonyms: | 3-Thiopheneacetamide, N-[(5-chloro-2-propoxyphenyl)methyl]-N-[2-[4-[(2-propyn-1-ylamino)sulfonyl]phenyl]ethyl]-;N-[(5-chloro-2-propoxyphenyl)methyl]-N-(2-{4-[(pr
op-2-yn-1-yl)sulfamoyl]phenyl}ethyl)-2-(thiophen-
3-yl)acetamide;YQ128;YQ128,inhibit,YQ 128,Inhibitor,NOD-like Receptor (NLR),Interleukin Related,YQ-128 | | CAS: | 2454246-18-3 | | MF: | C27H29ClN2O4S2 | | MW: | 545.11 | | EINECS: | | | Product Categories: | | | Mol File: | 2454246-18-3.mol |  |
| | YQ128 Chemical Properties |
| Boiling point | 705.8±70.0 °C(Predicted) | | density | 1.287±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 250 mg/mL (458.62 mM) | | form | A crystalline solid | | pka | 9.32±0.50(Predicted) | | color | White to off-white |
| | YQ128 Usage And Synthesis |
| Biological Activity | YQ128 is a potent and selective second-generation NLRP3 inflammasome inhibitor with IC50 of 0.30 μM. YQ128 significantly and selectively inhibited the production of IL-1β, but not TNF-α. YQ128 can cross the blood-brain barrier to reach the central nervous system. YQ128 has anti-inflammatory activity. | | in vitro | YQ128 (0.3-100 μM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC 50 of 1.59 μM.
YQ128 (20 μM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.
Cell Viability Assay < td class="col1"> Cell Line: | Mouse peritoneal macrophages | | Concentration: | 0.3, 1.0, 3.0, 10, 30, 100 μM | | Incubation Time: | 30 mins | | Result: | Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC 50 of 1.59 μM. | | | in vivo | YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration.
YQ128 (oral ; 20 mg/kg) shows delayed gastrointestinal absorption with at max and c max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F oral < /sub> ) is estimated as 10%.
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd ss ) of 8.5 L/kg and rapid total clearance (CL tot ) of 41 mL/min/kg.
has been shown to trigger IL-1β production in a NLRP3-dependent manner in C57BL/6 mice. < /p> < tr> | Animal Model: | Sprague-Dawley rats (200-250 g) | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) | Administration: | Iv | | Result: | < td class="col2"> Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |
| | YQ128 Preparation Products And Raw materials |
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