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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
INCB8761
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1341224-83-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1726.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥600.0 |
| 规格： | 5 mg | 产品价格： | ￥1380.0 |
| 规格： | 10 mg | 产品价格： | ￥2220.0 |
| 规格： | 25 mg | 产品价格： | ￥3800.0 |
| 规格： | 50 mg | 产品价格： | ￥5330.0 |
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PF-4136309
CAS No. : 1341224-83-6
MCE 国际站：PF-4136309
产品活性：PF-4136309 是一种高效，选择性，可口服的 CCR2 拮抗剂，能够抑制人，小鼠和大鼠 CCR2，IC50 值分别为 5.2 nM，17 nM 和 13 nM。
研究领域：GPCR/G Protein | Immunology/Inflammation
作用靶点：CCR
In Vitro: PF-4136309 is potent in human chemotaxis activity (IC50=3.9 nM) and in the whole blood assay (IC50=19 nM), with IC50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM.
In Vivo: PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species.
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文献和实验用量限制了这一治疗方案的广泛应用。目前诱导多能干细胞（iPSC）分化为产生胰岛素的 β 样细胞是一项重大进展。2021 年美国食品和药物管理局（FDA）已授予 VX-880（一种 iPSC 细胞在体外诱导分化而来的胰岛 β 细胞）快速通道指定，目前已启动 VX-880 的临床试验，用于治疗严重低血糖和低血糖意识受损的 1 型糖尿病（T1D）患者。在 2023 年 6 月举办的美国糖尿病协会 (ADA) 第 83 届科学会议上公布了正在进行的 VX-880 临床试验的积极结果：所有接受 VX-880 治疗的患者均
Metallomics Using Inductively Coupled Plasma Mass Spectrometry
proteins from a DEAE anion‐exchange column showing molybdenum (‐x‐) and protein (⋅⋅ o ⋅⋅) concentrations. Box shows fractions pooled for PF1972 purification (adapted from Cvetkovic et al., ). View Image
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