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D 927

Pricing Availability   Qty
化学名: 3-Fluoro-4-[[7-[2-(2-methoxyethoxy)phenyl]thieno[2,3-d]pyridazin-4-yl]amino]benzeneacetamide
纯度: ≥98% (HPLC)
说明书
引用文献
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生物活性 for D 927

D 927 is a molecular glue increasing the binding affinity of phosphoinositide 3-kinase α (PI3Kα) catalytic subunit p110α (Kd = 5.6 μM) to canonical small guanosine triphosphatase RAS proteins and to RRAS, RRAS2, and MRAS by three orders of magnitude.

D 927 binds to the RAS-binding domain of p110α, stabilizing the secondary structures of the PI3Kα in a RAS-binding conformation and forming direct interactions with RAS residues tyrosine-40 and arginine-41.

In vivo, D 927 mimicks the effects of insulin, rapidly lowering blood glucose concentrations, enhancing glucose metabolism in normal and Zucker fatty rats, and improving hyperglycemia in models of type 1 and type 2 diabetes, even in insulin-deficient diabetic animals. D 927 is orally bioavailable.

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技术数据 for D 927

分子量 452.5
公式 C23H21FN4O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2253733-37-6
PubChem ID 138454789
InChI Key GWLCNGUGZNFYHI-UHFFFAOYSA-N
Smiles O=C(CC1=CC=C(C(F)=C1)NC2=C3C=CSC3=C(C4=CC=CC=C4OCCOC)N=N2)N

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for D 927

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 9.05 20
ethanol 45.25 100

制备储备液 for D 927

以下数据基于产品分子量 452.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.21 mL 11.05 mL 22.1 mL
5 mM 0.44 mL 2.21 mL 4.42 mL
10 mM 0.22 mL 1.1 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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产品说明书 for D 927

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参考文献 for D 927

参考文献是支持产品生物活性的出版物。

Terayama et al (2025) Molecular glues that facilitate RAS binding to PI3Ká promote glucose uptake without insulin. Science 389 402 PMID: 40705882


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