YQ128
- Product Name
- YQ128
- CAS No.
- 2454246-18-3
- Chemical Name
- YQ128
- Synonyms
- YQ128;YQ128, 10 mM in DMSO;YQ128,inhibit,YQ 128,Inhibitor,NOD-like Receptor (NLR),Interleukin Related,YQ-128;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
- CBNumber
- CB98199880
- Molecular Formula
- C27H29ClN2O4S2
- Formula Weight
- 545.11
- MOL File
- 2454246-18-3.mol
YQ128 Property
- 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
- InChIKey
- SFPYRFRNYALLHS-UHFFFAOYSA-N
- SMILES
- C1SC=CC=1CC(N(CC1=CC(Cl)=CC=C1OCCC)CCC1=CC=C(S(NCC#C)(=O)=O)C=C1)=O
N-Bromosuccinimide Price
- Product number
- CS-0106043
- Product name
- YQ128
- Purity
- 99.65%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0106043
- Product name
- YQ128
- Purity
- 99.65%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0106043
- Product name
- YQ128
- Purity
- 99.65%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
- Product number
- CS-0106043
- Product name
- YQ128
- Purity
- 99.65%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
YQ128 Chemical Properties,Usage,Production
Uses
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity[1]. YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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
| 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) Iv Result: < td class="col2"> Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration.
IC 50
NLRP3: 0.30 μM (IC50); IL-1β
YQ128 Preparation Products And Raw materials
Raw materials
Preparation Products
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