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

Chemical Structure : Tirzepatide

CAS No.: 2023788-19-2

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Tirzepatide (LY3298176)

货号: PC-72629Not For Human Use, Lab Use Only.

Tirzepatide (LY3298176) is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist, binds both receptor with high affinity (GIPR Ki=0.135; GLP-1R Ki=4.23 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tirzepatide (LY3298176) is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist, binds both receptor with high affinity (GIPR Ki=0.135; GLP-1R Ki=4.23 nM).
Tirzepatide (LY3298176) is comparable to native GIP for the GIPR and approximately 5-fold weaker than native GLP-1 for the GLP-1R.
Tirzepatide (LY3298176) potently stimulates cAMP accumulation by either receptor (GIPR EC50=0.0224 nM; GLP-1R EC50=0.934 nM) in signaling studies using cell lines with recombinantly expressed GIPR or GLP-1R.
Tirzepatide (LY3298176) is less potent than the selective GLP-1RA semaglutide (Cat. PC-73177) (GLP-1R Ki=1.97 nM; cAMP EC50=0.0571 nM), and has minimal activity on the closely related glucagon receptor.
Tirzepatide (LY3298176) can induce glucose-dependent insulin secretion in vitro and in vivo through either the GIPR or the GLP-1R.

物理化学性质&存储条件

分子量 4813.45
分子式 C225H348N48O68
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

Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS-NH2

参考文献

1. Frias JP, et al. Lancet. 2018 Nov 17;392(10160):2180-2193.

2. Frias JP, et al. Diabetes Obes Metab. 2020 Jun;22(6):938-946.

3. Coskun T, et al. Mol Metab. 2018 Dec;18:3-14.

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