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Dulaglutide (Activated main chain) is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. Dulaglutide binds to glucagon-like peptide 1 receptors, slowing gastric emptying and increases insulin secretion by pancreatic Beta cells. Simultaneously the compound reduces the elevated glucagon secretion by inhibiting alpha cells of the pancreas. GLP-1 is normally secreted by L cells of the gastrointestinal mucosa in response to a meal.
Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 3213.2 |
| Formula | |
| CAS Number | 923950-08-7 |
| Purity | >98% |
| Solubility | Soluble in water |
| Storage | at -20°C |
[2] Nadkarni P, et al. Prog Mol Biol Transl Sci. Regulation of glucose homeostasis by GLP-1.
| Related Glucagon Receptor Products |
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| LSN3318839
LSN3318839 is an orally active allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R). |
| GLP-1(7-36), amide TFA
TFA is a major intestinal hormone that stimulates insulin secretion by pancreatic beta cells in response to glucose. |
| GLP-1(7-37)
Glp-1 (7-37) is an intestinal insulin hormone that enhances glucose-induced insulin secretion. |
| PF-06882961
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) agonist. |
| Teduglutide
Teduglutide is a glucagon-like peptide-2 (GLP- 2) receptor agonist used for the treatment of short-bowel syndrome. |
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