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Retatrutide

SKU: orb1981169

Description

Retatrutide (LY3437943) is a triple agonist targeting the GLP-1, GIP, and glucagon receptors. It is a research compound used in metabolic studies, particularly for investigating obesity mechanisms in preclinical in vivo and in vitro models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number2381089-83-2
MW4732.09
Purity98.31%
FormulaC221H342N46O68
SMILESCC[C@H](C)C(C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N3CCC[C@H]3C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)CC[C@@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@](C)(CC(C)C)NC(=O)C([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CC=C(C=C7)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC8=CC=CC=C8)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C(C)(C)NC(=O)[C@H](CC9=CC=C(C=C9)O)N
TargetGlucagon Receptor
SolubilityH2O:30 mg/mL (6.34 mM);DMSO:30 mg/mL (6.34 mM)

Bioactivity

Target IC50
GLP1 receptor:0.775 nM (EC50, human)|GLP1 receptor:0.794 nM (EC50, mouse)|GLP1 receptor:7.2 nM (Ki, human)|GLP1 receptor:1.3 nM (Ki, mouse)|GCGR:5.79 nM (EC50, human)|GCGR:2.32 nM (EC50, mouse)|GCGR:73 nM (Ki, mouse)|GCGR:5.6 nM (Ki, human)|GIPR:0.0643 nM (EC50, human)|GIPR:0.057 nM (Ki, human)|GIPR:2.8 nM (Ki, mouse)|GIPR:0.191 nM (EC50, mouse)
In Vivo
In vivo, Retatrutide (LY3437943) engages with GCGR and, when administered through subcutaneous injection at a single dose of 0.47 mg/kg, improves glucose tolerance in an ipGTT (intraperitoneal glucose tolerance test) through activation of GIP or GLP-1 receptors. With subcutaneous injections at 10 mL/kg every 3 days in a cycle sustained for 21 days, Retatrutide leads to significant weight reduction and increased energy expenditure through activation of glucagon receptor.
In Vitro
Retatrutide (LY3437943) exhibits activity against human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM, respectively. For mouse GCGR, GIPR, and GLP-1R, Retatrutide shows activity with EC50 values of 2.32, 0.191, and 0.794 nM, respectively. In terms of binding affinity, Retatrutide has Ki values of 5.6, 0.057, and 7.2 nM for human GCGR, GIPR, and GLP-1R, respectively. Similarly, for mouse GCGR, GIPR, and GLP-1R, Retatrutide exhibits binding affinity with Ki values of 73, 2.8, and 1.3 nM, respectively.

Storage & Handling

Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

GLP-1, GlucagonReceptor, Glucagon Receptor, GCGR, LY3437943

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Key Properties

No computed properties available.

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Retatrutide (orb1981169)

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1 mg
¥ 3,770.00
5 mg
¥ 8,710.00
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