INCB8761(PF-4136309)
- CAS号:1341224-83-6
- 英文名:INCB8761(PF-4136309)
- 中文名:INCB8761(PF-4136309)
- CBNumber:CB62627975
- 分子式:C29H31F3N6O3
- 分子量:568.59
- MOL File:1341224-83-6.mol
- 沸点 :712.2±60.0 °C(Predicted)
- 密度 :1.40±0.1 g/cm3(Predicted)
- 储存条件 :Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- 溶解度 :Soluble in DMSO (up to at least 25 mg/ml)
- 形态 :solid
- 酸度系数(pKa) :13.17±0.46(Predicted)
- 颜色 :Off-white
- 稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- 海关编码 :2933998090
INCB8761(PF-4136309)性质、用途与生产工艺
- 生物活性 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。
-
靶点
Human CCR2
5.2 nM (IC 50 )
Mouse CCR2
13 nM (IC 50 )
Rat CCR2
17 nM (IC 50 )
-
体外研究
PF-4136309 is potent in human chemotaxis activity (IC 50 =3.9 nM) and in the whole blood assay (IC 50 =19 nM), with IC 50 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 IC 50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC 50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC 50 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.
-
体内研究
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 (T max ) 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.
- 公司名称:Musechem
- 联系电话:+1-800-259-7612
- 电子邮件:info@musechem.com
- 国家:美国
- 产品数:4662
- 优势度:60
- 公司名称:InvivoChem
- 联系电话:+1-708-310-1919 +1-13798911105
- 电子邮件:sales@invivochem.cn
- 国家:美国
- 产品数:6393
- 优势度:58
- 公司名称:Cckinase, Inc.
- 联系电话:+1 (732)236-3202
- 电子邮件:sales@cckinase.com
- 国家:美国
- 产品数:2738
- 优势度:58
- 公司名称:BOC Sciences
- 联系电话:+1-631-485-4226
- 电子邮件:inquiry@bocsci.com
- 国家:美国
- 产品数:19553
- 优势度:58
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354
- 电子邮件:support@targetmol.com
- 国家:美国
- 产品数:19973
- 优势度:58
- 公司名称:ApexBio技术
- 联系电话:--
- 电子邮件:sales@apexbt.com
- 国家:美国
- 产品数:6254
- 优势度:58
- 公司名称:Focus Biomolecules
- 联系电话:--
- 电子邮件:sales@focusbiomolecules.com
- 国家:美国
- 产品数:1284
- 优势度:58
- 公司名称:CAYMAN
- 联系电话:--
- 电子邮件:cayman@caymanchem.com
- 国家:美国
- 产品数:6618
- 优势度:81
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58