YQ128
YQ128
CAS: 2454246-18-3
Molecular Formula: C27H29ClN2O4S2
YQ128 - Names and Identifiers
YQ128 - Physico-chemical Properties
| Molecular Formula | C27H29ClN2O4S2 |
| Molar Mass | 545.11 |
| Density | 1.287±0.06 g/cm3(Predicted) |
| Boling Point | 705.8±70.0 °C(Predicted) |
| pKa | 9.32±0.50(Predicted) |
| In vitro study | 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 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 study | 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 a t max and c max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F oral ) 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. YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice. Animal Model: Sprague-Dawley rats (200-250 g) Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: Iv Result: Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |
YQ128 - Reference Information
| biological activity | YQ128 is effective, selective second-generation NLRP3 inflammatory body inhibitor, IC50 is 0.30 µM. YQ128 significantly and selectively inhibited IL-1β production, but not TNF-α production. YQ128 can cross the blood-brain barrier to reach the central nervous system. YQ128 has anti-inflammatory activity. |
| target | NLRP3 0.30 μM (IC 50 ) IL-1β |
| in vitro research | 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 m. yq128 (20 m; 2 hours) shows no significant toxic effects on hCMEC/D3 cells. Cell Viability Assay Cell Line: Mouse peritoneal macrophages Concentration: 0.3, 1.0, 3.0, 10, 30,100 m 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. |
| 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. Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |
| in vivo study | 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 a t max and c max of 12 h and 73 ng/ml, respectively. oral bioavailability (f oral ) is estimated as 10%. yq128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (vdss) of 8.5 l/kg and rapid total clearance (cl tot ) of 41 mL/min/kg. yq128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mICE. Animal Model: sprague-Dawley rats (200-250g) Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: Iv Result: Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |
| Animal Model: | Sprague-Dawley rats (200-250 g) |
| Dosage: | 20 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Iv |
Last Update：2024-04-09 01:59:58
Supplier List
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: YQ128 Visit Supplier Webpage Request for quotationCAS: 2454246-18-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
YQ128
2975-71-5
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
868166-28-3
313506-81-9
6-hydroxysporotricale
15997-44-1
20,21-[(tert-Butylboranediyl)bis(oxy)]-5α-pregn-17(20)-en-3-one
N-(4-hydroxy-1-naphthyl)-2,5-dimethylbenzenesulfonamide
2-[2-(4-tert-butylphenyl)sulfinylphenyl]-4-phenyl-4,5-dihydrooxazole
2975-71-5
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
868166-28-3
313506-81-9
6-hydroxysporotricale
15997-44-1
20,21-[(tert-Butylboranediyl)bis(oxy)]-5α-pregn-17(20)-en-3-one
N-(4-hydroxy-1-naphthyl)-2,5-dimethylbenzenesulfonamide
2-[2-(4-tert-butylphenyl)sulfinylphenyl]-4-phenyl-4,5-dihydrooxazole