1. Metabolic Enzyme/Protease
  2. Lipocalin Family
  3. BPN-14136

BPN-14136 是一种口服有效的视黄醇结合蛋白 4 (RBP4) 抑制剂。BPN-14136 抑制视黄醇与 RBP4 的结合,其 IC50 为 12.8 nM。BPN-14136 可抑制视黄醇依赖性 RBP4-转甲状腺素蛋白的相互作用 (IC50 = 43.6 nM),并在体内降低循环血浆中的 RBP4 水平。BPN-14136 可减少视网膜色素上皮细胞中细胞毒性双视黄醇的形成。BPN-14136 可用于萎缩性年龄相关性黄斑变性和斯塔加特病的研究。

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BPN-14136

BPN-14136 Chemical Structure

CAS No. : 1628945-93-6

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查看 Lipocalin Family 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BPN-14136 is an orally effective retinol-binding protein 4 (RBP4) inhibitor. BPN-14136 inhibits the binding of retinol to RBP4 with an IC50 of 12.8 nM. BPN-14136 inhibits retinol-dependent RBP4-transthyretin interaction (IC50 = 43.6 nM) and reduces circulating plasma RBP4 levels in vivo. BPN-14136 decreases the formation of cytotoxic bisretinoids in retinal pigment epithelial cells. BPN-14136 can be used for the research of atrophic age-related macular degeneration and Stargardt disease[1].

体外研究
(In Vitro)

BPN-14136 (Compound 33) (10 μM; 30 min) 在人源和大鼠肝微粒体实验中表现出极佳的稳定性,在 10 μM 浓度下孵育 30 分钟后,剩余率分别为 94% 和 93%[1]
BPN-14136 具有良好的体外 ADMET 特征,包括高溶解度、极低的肝脏清除率、无显著的 CYP 或 hERG 抑制作用、高血浆蛋白结合率以及高 MDR1-MDCK 通透性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUClast AUCINF_obs Bioavailability C0 CL Vss
Rat[1] 5.1 μmol/Kg i.v. / / 22.0 h 795 μM·h 1017 μM·h / 58.6 μM 5.06 mL/min/kg 156 mL/kg
Rat[1] 12.7 μmol/Kg p.o. 62.2 μM 2.67 h 38.8 h 2011 μM·h 3636 μM·h 143 % / / /
体内研究
(In Vivo)

BPN-14136 (Compound 33) (5 mg/kg;口服;每日单次给药,连续 7 天) 可显著降低血浆 RBP4 水平,单次给药后降低 85%,连续 7 天每日给药后降低 95%[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, adult, drug-naive)[1]
Dosage: 5 mg/kg (single dose); 5 mg/kg (7-day daily dosing)
Administration: p.o.; single dose; 7 days
Result: Induced an 85% maximum decrease in plasma RBP4.
Induced an approximately 95% reduction in plasma RBP4.
分子量

391.39

Formula

C20H20F3N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BPN-14136
目录号:
HY-182385
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