PROTAC^®(H-PGDS)-7

Cat. No. 8004 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent hematopoietic prostaglandin D₂ synthase Degrader (PROTAC^®)

化学名： N-[4-[4-[[4-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-1-piperazinyl]carbonyl]-1-piperidinyl]phenyl]-2-phenoxy-5-pyrimidinecarboxamide

纯度： ≥98% (HPLC)

文献 (2)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PROTAC^®(H-PGDS)-7

PROTAC^®(H-PGDS)-7 is a potent Degrader of hematopoietic prostaglandin D₂ synthase (H-PGDS; DC₅₀ = 17pM after 24 hours). Comprises the H-PGDS inhibitor TFC-007 (Cat. No. 5108) directly linked to E3 ligase cereblon. Suppresses prostaglandin D₂ production in vitro and in vivo.

PROTAC^®(H-PGDS)-8 negative control (Cat. No. 8005) also available.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

许可信息

Sold under license from National Institute of Health Sciences, Japan and Tsuzuki Gakuen.

技术数据 for PROTAC^®(H-PGDS)-7

分子量	742.79
公式	C₄₀H₃₈N₈O₇
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	2761281-50-7
PubChem ID	162679258
InChI Key	KQNXUQJGOJWQGL-UHFFFAOYSA-N
Smiles	O=C(C1=CN=C(OC2=CC=CC=C2)N=C1)NC3=CC=C(N4CCC(CC4)C(N5CCN(CC5)C(C=CC=C6C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)C=C3

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 PROTAC^®(H-PGDS)-7

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	74.28	100

制备储备液 for PROTAC^®(H-PGDS)-7

以下数据基于产品分子量 742.79。 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	1.35 mL	6.73 mL	13.46 mL
5 mM	0.27 mL	1.35 mL	2.69 mL
10 mM	0.13 mL	0.67 mL	1.35 mL
50 mM	0.03 mL	0.13 mL	0.27 mL

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产品说明书 for PROTAC^®(H-PGDS)-7

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PROTAC^®(H-PGDS)-7

参考文献是支持产品生物活性的出版物。

Osawa et al (2023) CRBN ligand expansion for hematopoietic prostaglandin D₂ synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles. Bioorg.Med.Chem. 84 117259 PMID: 37018877

Murakami et al (2022) Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D₂ synthase. RSC Med.Chem. 13 1495 PMID: 36561070

Yokoo et al (2021) Discovery of a highly potent and selective Degrader targeting hematopoietic prostaglandin D synthase via in silico design. J.Med.Chem. 64 15868 PMID: 34652145

If you know of a relevant reference for PROTAC^®(H-PGDS)-7, please let us know.

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关键词: PROTAC®(H-PGDS)-7, PROTAC®(H-PGDS)-7 supplier, PROTACHPGDS7, PROTAC, protacs, active, degrader, degraders, hematopoietic, prostaglandin, D2, synthase, cereblon, E3, ligase, proteolysis, targeting, chimera, HPGDS, Other, Synthases/Synthetases, Degraders, 8004, Tocris Bioscience

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该领域的文献

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TPD and Induced Proximity Research Product GuideUpdated

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

Active Degraders
TAG Degradation Platform
Degrader Building Blocks
Assays for Protein Degradation
Induced Proximity Tools

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia