GnRH-R antagonist-2
GnRH-R antagonist-2 (Compound 44c) is a Gonadotropin releasing hormone receptor (GnRH-R) antagonist with IC50s of 43 and 88 nM for rat and human GnRH-R, respectively. GnRH-R antagonist-2 can be used for hormone dependent diseases such as endometriosis, breast and prostate cancer research.
For research use only. We do not sell to patients.
- CAS No.: 1000819-21-5
- Formula: C37H50N4O3S
- Molecular Weight:630.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
88 nM
Compound: 44
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Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
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[PMID: 17937987] |
| Pituitary gland cell | IC50 |
220 nM
Compound: 44
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Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
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[PMID: 17937987] |
Chemical Information
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CAS No. 1000819-21-5
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Molecular Weight 630.88
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Formula C37H50N4O3S
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SMILES
O=C(C1CCN(CC1C)CCC2=C(C3=CC(C)=CC(C)=C3)NC4=C2C=C(C(C)(C)C(N5C6CCC5CC6)=O)S4)N7CCOCC7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GnRH-R antagonist-2 Related Classifications
HY-178418 Related Classifications
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