GnRH-R antagonist 1
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
For research use only. We do not sell to patients.
- CAS No.: 2826273-90-7
- Formula: C31H28F5N7O6S
- Molecular Weight:721.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
In Vitro
GnRH-R antagonist 1 has a 140-fold higher cell permeability than Relugolix and exhibits favorable stability in human and mouse microsome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
GnRH-R antagonist 1 (12 mg/kg; p.o.; single) shows favorable pharmacokinetic properties and high oral bioavailability with a F% value of 44.7%[1].
GnRH-R antagonist 1 (12 mg/kg; p.o.; single) inhibits circulating testosterone levels in rats (lasts for more than 24 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult Sprague-Dawley rats (200-250 g)[1].
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Dosage:30 mg/kg
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Administration:Oral administration; single daily for 7 days.
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Result:Showed no ames toxicity.
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Animal Model:Adult Sprague-Dawley rats (200-250 g)[1].
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Dosage:1 mg/kg (for i.v.); 12 mg/kg (for p.o.)
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Administration:Intravenous administration ;oral administration; single.
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Result:Exhibited clear and significnt suppressive effects on circulating testosterone levels in rats, and the suppressive effects lasted for more than 24 h.
1.19 Pharmacokinetic Parameters of GnRH-R antagonist 1 in Adult Sprague-Dawley rats[1].
IV (1 mg/kg) PO (12 mg/kg) Tmax (h) - 1.13 Cmax (nmol/L) 3918.8 920.1 AUCLast (nmol/L•h) 1374.6 7370.6 CL (L/h/kg) 1.05 - t1/2 (h) 2.79 4.86 F (%) - 44.7
Chemical Information
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CAS No. 2826273-90-7
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Molecular Weight 721.65
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Formula C31H28F5N7O6S
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SMILES
O=C(NOC)NC1=CC=C(C(S2)=C(CN(C)CCOC(F)(F)F)C(C(N3C4=NN=C(OC)C=C4)=O)=C2N(CC5=C(F)C=CC=C5F)C3=O)C=C1
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GnRH-R antagonist 1 Related Classifications
HY-151247 Related Classifications
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