NBI-42902
Based on 1 Customer Validation
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
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- Purity: 98.65%
- CAS No.: 352290-60-9
- 화학식: C27H24F3N3O3
- 분자량:495.49
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.59 nM
Compound: 2a; NBI-42902
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Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
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[PMID: 27608177] |
| HEK293 | IC50 |
87 nM
Compound: 2a; NBI-42902
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Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b
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[PMID: 27608177] |
| RBL-1 | IC50 |
2.8 nM
Compound: 4a, NBI-42902
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Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
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[PMID: 19006286] |
NBI-42902 (0-1000 nM) is quite sensitive to the relatively conservative sequence changes between species, with IC50 values of 0.79 nM (human), 10 nM (macaque), 400 nM (dog), 200 nM (rabbit) for the GnRH receptors[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-stimulated Ca2+ flux in RBL cells with a mean IC50 value of 3.6 nM[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-induced IP accumulation competitively in RBL cells[1].
NBI-42902 (1 nM-1 μM, 5 min) blocks GnRH-stimulated ERK1/2 phosphorylation completely in CHO-GnRHR cells with an IC50 value of 5.22 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO-GnRHR
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Concentration:1 nM-1 μM
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Incubation Time:5 min
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Result:Blocked GnRH (1 nM)-stimulated ERK1/2 phosphorylation completely in a dose-dependent manner, with an IC50 value of 5.22 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Castrated macaques[1]
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Dosage:10, 40, 100 mg/kg
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Administration:Oral administration (p.o.)
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Result:Inhibited serum LH with dose dependent.
Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.
Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
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Animal Model:Castrated macaques[1]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.)
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Result:Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
Chemical Information
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CAS No. 352290-60-9
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Appearance Solid
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분자량 495.49
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화학식 C27H24F3N3O3
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Color White to off-white
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SMILES
O=C1N(C[C@H](N)C2=CC=CC=C2)C(C(C3=CC=CC(OC)=C3F)=C(C)N1CC4=C(F)C=CC=C4F)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (201.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.05 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.05 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0182 mL | 10.0910 mL | 20.1820 mL | 50.4551 mL |
| 5 mM | 0.4036 mL | 2.0182 mL | 4.0364 mL | 10.0910 mL | |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0182 mL | 5.0455 mL | |
| 15 mM | 0.1345 mL | 0.6727 mL | 1.3455 mL | 3.3637 mL | |
| 20 mM | 0.1009 mL | 0.5046 mL | 1.0091 mL | 2.5228 mL | |
| 25 mM | 0.0807 mL | 0.4036 mL | 0.8073 mL | 2.0182 mL | |
| 30 mM | 0.0673 mL | 0.3364 mL | 0.6727 mL | 1.6818 mL | |
| 40 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2614 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.0091 mL | |
| 60 mM | 0.0336 mL | 0.1682 mL | 0.3364 mL | 0.8409 mL | |
| 80 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6307 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5046 mL |
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