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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
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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