The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein R1, AA1, AA2, LysR, X and Y are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Glucagon-like peptide-1 (GLP-1) ...
CONCLUSION: The GLP-1 receptor antagonist exendin(9-39) labelled with (125)I-BH at lysine 19 is an excellent GLP-1 radioligand that identifies human and rat GLP-1 receptors in normal and tumoural tissues. It may therefore be the molecular basis to develop suitable GLP-1 receptor antagonist...
Type 2 diabetes (T2D) is a complex and progressive disease requiring polypharmacy to manage hyperglycaemia and cardiovascular risk factors. However, most patients do not achieve combined treatment goals. To address this therapeutic gap, we have developed
This is suggested by the finding that the inhibitory effect of GLP-1 was abolished by the GLP-1 receptor antagonist exendin (9-39). As will be discussed below, the low α cell GLP-1 receptor density has important functional implications and is, in fact, a prerequisite for its inhibitory ...
TargetMol 1ml 99.58%;1 mL * 10 mM (in DMSO) ￥1,420.00 ￥1,136.00 购买 TargetMol 1mg 99.58% ￥538.00 ￥430.00 购买 阿拉丁 1mg ≥98%(HPLC) ￥799.90 ￥640.00 购买 GLPG0974用途 GLPG0974是游离脂肪酸受体-2 (free fatty acid receptor-2 (FFA2/GPR43)) 拮抗剂,IC50 值为 9 nM。 产品...
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides ...
(2006) “Design of a long acting peptide functioning as both a glucagon-like peptide-1 receptor agonist and a glucagon receptor antagonist.” Journal of Biological Chemistry. 281(18):12506-12515. Pocai (Dec. 14, 2013) “Action and therapeutic potential of oxyntomodulin,” Molecular Metabolism...
GLP-1 receptor antagonist exendin-(9-39) elevates fasting blood glucose levels in congenital hyperinsulinism owing to inactivating mutations in the ATP-sensitive K+ channel. Diabetes 2012; 61: 2585-91.Calabria AC, Li C, Gallagher PR, Stanley CA, De Leon DD. GLP-1 receptor antagonist ...
GLP-1 RECEPTOR ANTAGONIST FOR USE IN THE TREATMENT OF CONGENITAL HYPERINSULINISMAn antagonist of the Glucagon Like Peptide-1 (GLP-1) receptor, or a composition of exendin-(9-39), for use in the treatment of congenital hyperinsulinism.
These hypotheses are supported by studies employing the GLP-1 receptor antagonist, exendin(9-39), where opposite effects were seen. In humans, administered GLP-1 has a satiating effect, and when given by continuous subcutaneous infusion over a 6 weeks regime, patients with diabetes exhibited a ...