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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
| Molecular Weight | 3213.2 |
| CAS Number | 923950-08-7 |
| Solubility (25°C) | Soluble in water |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[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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Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM. |
| Semaglutide TFA
Semaglutide TFA, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide TFA has the potential for type 2 diabetes treatment. |
| MK 0893
MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. |
| Lixisenatide acetate
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM). |
| GLP-1(7-36), amide acetate
GLP-1(7-36), amide acetate is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells. |
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