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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-Danuglipron
Danuglipron

Chemical Structure : Danuglipron

CAS No.: 2230198-02-2

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Danuglipron (PF-06882961, PF 06882961)

货号: PC-72210Not For Human Use, Lab Use Only.

Danuglipron (PF-06882961) is a potent, selective, non-peptide and orally bioavailable agonist of glucagon-like peptide-1 receptor (GLP-1R) with cAMP production EC50 of 1.1 nM.

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10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg ￥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Danuglipron (PF-06882961) is a potent, selective, non-peptide and orally bioavailable agonist of glucagon-like peptide-1 receptor (GLP-1R) with cAMP production EC50 of 1.1 nM.
Danuglipron (PF-06882961) is a full agonist (EC50 = 13 nM) in the CS cAMP assay.
Danuglipron (PF-06882961) is a partial agonist in recruiting βArr2 (EC50 = 490 nM; Emax = 36%), exhibits subtle bias for cAMP, relative to βArr1 recruitment.
Danuglipron (PF-06882961) shows Ki value of 360 nM using a competition binding assay.
Danuglipron (PF-06882961) does not activate the rodent GLP-1R.
Danuglipron (PF-06882961) demonstrated beneficial changes during a recently reported multiple-dose study in volunteers with T2DM.

 

 

物理化学性质&存储条件

分子量 555.61
分子式 C31H30FN5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-2-((4-(6-((4-Cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid

参考文献

1. Zhang X, et al. Mol Cell. 2020 Nov 5;80(3):485-500.e7.

2. Choe HJ, et al. Endocrinol Metab (Seoul). 2021 Feb;36(1):22-29.

3. Saxena AR, et al. Nat Med. 2021 Jun;27(6):1079-1087.

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